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Comprehensive survey of combinatorial libraries with undisclosed biological activity: 1992–1997

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References

  1. a. Dolle, R.E., Comprehensive survey of chemical libraries yielding enzyme inhibitors, receptor agonists and antagonists, and other biologically active agents: 1992 through 1997, Mol. Diversity, 3 (1998) 199–233. b. For a review of 1998 libraries see: Dolle, R.E. and Nelson Jr., K.H., Comprehensive survey of combinatorial library synthesis: 1998, J. Comb. Chem., 1 (1999) 235–282.

    Google Scholar 

  2. Adamczyk, M. and Fishpaugh, J.R., A solid supported synthesis of thiol esters, Tetrahedron Lett., 37 (1996) 4305–4308.

    Google Scholar 

  3. Arumugam, V., Routledge, A., Abell, C. and Balasubramanian, S., Synthesis of 2-oxindole derivatives via the intramolecular Heck reaction on solid support, Tetrahedron Lett., 38 (1997) 6473–6476.

    Google Scholar 

  4. Atuegbu, A., Maclean, D., Nguyen, C., Gordon, E.M. and Jacobs, J.W., Combinatorial modification of natural products: Preparation of unencoded and encoded libraries of Rauwolfia alkaloids, Bioorg. Med. Chem., 4 (1996) 1097–1106.

    Google Scholar 

  5. Backes, B.J. and Ellman, J.A., Carbon-carbon bond-forming methods on solid support. Utilization of Kenner's ‘safety-catch’ linker, J. Am. Chem. Soc., 116 (1994) 11171–11172.

    Google Scholar 

  6. Backes, B.J., Virgilio, A.A. and Ellman, J.A., Activation method to prepare a highly reactive acylsulfonamide ‘safety-catch’ linker for solid-phase synthesis, J. Am. Chem. Soc., 118 (1996) 3055–3056.

    Google Scholar 

  7. Bailey, N., Dean, A.W., Judd, D.B., Middlemiss, D., Storer, R. and Watson, S.P., A convenient procedure for the solution phase preparation of 2-aminothiazole combinatorial libraries, Bioorg. Med. Chem. Lett., 6 (1996) 1409–1414.

    Google Scholar 

  8. Baldino, C.M., Casebier, D.S., Caserta, J., Slobodkin, G., Tu, C. and Coffen, D.L., Convergent parallel synthesis, Synlett., (1997) 488–490.

  9. Baldwin, J.J., Burbaum, J.J., Henderson, I. and Ohlmeyer, M.H.J., Synthesis of a small molecule combinatorial library encoded with molecular tags, J. Am. Chem. Soc., 117 (1995) 5588–5589.

    Google Scholar 

  10. Baldwin, J.J., Design, synthesis and use of binary encoded synthetic chemical libraries, Mol. Diversity, 2 (1996) 81–88.

    Google Scholar 

  11. Bauer, U., Ho, W.-B. and Koskinen, A.M.P., A novel linkage for the solid-phase synthesis of hydroxamic acids, Tetrahedron Lett., 38 (1997) 7233–7236.

    Google Scholar 

  12. Beaver, K.A., Siegmund, A.C. and Spear, K.L., Application of the sulfonamide functional group as an anchor for solid phase organic synthesis (SPOS), Tetrahedron Lett., 37 (1996) 1145–1148.

    Google Scholar 

  13. Beebe, X., Schore, N.E. and Kurth, M.J., Polymer-supported synthesis of cyclic ethers: Electrophilic cyclization of isoxazolines, J. Org. Chem., 60 (1995) 4196–4203.

    Google Scholar 

  14. Beebe, X., Chiappari, C.L., Olmstead, M.M., Kurth, M.J. and Schore, N.E., Polymer-supported synthesis of cyclic ethers: Electrophilic cyclization of tetrahydrofuroisoxazolines, J. Org. Chem., 60 (1995) 4204–4212.

    Google Scholar 

  15. Berk, S.C. and Chapman, K.T., Spatially arrayed mixture (SPAM) technology: Synthesis of two-dimensionally indexed orthogonal combinatorial libraries, Bioorg. Med. Chem. Lett., 7 (1997) 837–842.

    Google Scholar 

  16. Bhalay, G., Blaney, P., Palmer, V.H. and Baxter, A.D., Solid-phase synthesis of diverse tetrahydro-1,4-benzodiazepine-2-ones, Tetrahedron Lett., 38 (1997) 8375–8378.

    Google Scholar 

  17. Bicknell, A.J. and Hird, N.W., Synthesis of a highly functionalized rigid template by solid phase azomethine ylide cycloaddition, Bioorg. Med. Chem. Lett., 6 (1996) 2441–2444.

    Google Scholar 

  18. Boehm, T.L. and Showalter, H.D.H., Development of a novel silyl ether linker for solid-phase organic synthesis, J. Org. Chem., 61 (1996) 6498–6499.

    Google Scholar 

  19. Boger, D.L., Tarby, C.M., Myers, P.L. and Caporale, L.H., Generalized dipeptidomimetic template: Solution phase parallel synthesis of combinatorial libraries, J. Am. Chem. Soc., 118 (1996) 2109–2110.

    Google Scholar 

  20. Boger, D.L., Ozer, R.S. and Andersson, C.-M., Generation of targeted C2-symmetrical compound libraries by solution-phase combinatorial chemistry, Bioorg. Med. Chem. Lett., 7 (1997) 1903–1908.

    Google Scholar 

  21. Boger, D.L., Chai, W., Ozer, R.S. and Anderson, C.-M., Solution-phase combinatorial synthesis via the olefin metathesis reaction, Bioorg. Med. Chem. Lett., 7 (1997) 463–468.

    Google Scholar 

  22. Bolton, G.L., Solid-phase synthesis of azabicyclo[4.3.0]-nonen-8-one amino acid derivatives via intramolecular Pauson-Khand cyclization, Tetrahedron Lett., 37 (1996) 3433–3436.

    Google Scholar 

  23. Bolton, G.L., Hodges, J.C. and Rubin, J.R., Solid-phase synthesis of fused bicyclic amino acid derivatives via intramolecular Pauson-Khand cyclization: Versatile scaffolds for combinatorial chemistry, Tetrahedron, 53 (1997) 6611–6634.

    Google Scholar 

  24. (a) Boojamra, C.G., Burow, K.M., Thompson, L.A. and Ellman, J.A., Solid-phase synthesis of 1,4-benzodiazepine-2,5-diones. Library preparation and demonstration of synthesis generality, J. Org. Chem., 62 (1997) 1240–1256. (b) Boojamra, C.G., Burow, K.M. and Ellman, J.A., An expedient and high-yielding method for the solid-phase synthesis of diverse 1,4-benzodiazepine-2,5-diones, J. Org. Chem., 60 (1995) 5742–5743.

    Google Scholar 

  25. Boyd, E.A., Chan, W.C. and Loh Jr., V.M., Multiple solid phase synthesis of (RS)-1-aminophosphinic acids, Tetrahedron Lett., 37 (1996) 1647–1650.

    Google Scholar 

  26. Bray, A.M., Chiefari, D.S., Valerio, R.M. and Maeji, N.J., Rapid optimization of organic reactions on solid phase using the Multipin approach: Synthesis of 4-aminoproline analogues by reductive amination, Tetrahedron Lett., 36 (1995) 5081–5084.

    Google Scholar 

  27. 27. Brown, S.D. and Armstrong, R.W., Synthesis of tetrasubstituted ethylenes on solid support via resin capture, J. Am. Chem. Soc., 118 (1996) 6331–6332.

    Google Scholar 

  28. Brown, A.R., Rees, D.C., Rankovic, Z. and Morphy, J.R., Synthesis of tertiary amines using a polystyrene (REM) resin, J. Am. Chem. Soc., 119 (1997) 3288–3295.

    Google Scholar 

  29. Brown, S.D. and Armstrong, R.W., Parallel synthesis of tamoxifen and derivatives on solid support via resin capture, J. Org. Chem., 62 (1997) 7076–7077.

    Google Scholar 

  30. Brown, E.G. and Nuss, J.M., Alkylation of Rink's amide linker on polystyrene resin: A reductive amination approach to modified amine-linkers for the solid phase synthesis of N-substituted amide derivatives, Tetrahedron Lett., 38 (1997) 8457–8460.

    Google Scholar 

  31. Brown, P.J., Hurley, K.P., Stuart, L.W. and Willson, T.M., Generation of secondary alkyl amines on solid support by borane reduction. Application to the parallel synthesis of PPAR ligands, Synthesis, (1997) 778–782.

  32. Buckman, B.O. and Mohan, R., Solid-phase synthesis of 1,3-dialkyl quinazoline-2,4-diones, Tetrahedron Lett., 37 (1996) 4439–4442.

    Google Scholar 

  33. Bunin, B.A. and Ellman, J.A., A general and expedient method for the solid-phase synthesis of 1,4-benzodiazepine derivatives, J. Am. Chem. Soc., 114 (1992) 10997–10998.

    Google Scholar 

  34. Bunin, B.A., Plunkett, M.J. and Ellman, J.A., The synthesis of a 1680 member 1,4-benzodiazepine library, New J. Chem., 21 (1997) 125–130.

    Google Scholar 

  35. Burgess, K., Ibarzo, J., Linthicum, D.S., Shin, H., Shitangkoon, A., Totani, R. and Zhang, A.J., Solid-phase syntheses of oligoureas, J. Am. Chem. Soc., 119 (1997) 1556–1564.

    Google Scholar 

  36. Burgess, K., Lim, D., Bois-Choussy, M. and Zhu, J., Rapid and efficient solid phase syntheses of cyclic peptides with endocyclic biaryl ether bonds, Tetrahedron Lett., 38 (1997) 3345–3348.

    Google Scholar 

  37. Cao, X. and Mjalli, A.M.M., Combinatorial method for the synthesis of α-hydroxy phosphonates on Wang resin, Tetrahedron Lett., 37 (1996) 6073–6076.

    Google Scholar 

  38. Chen, C., Randall, L.A.A., Miller, R.B., Jones, A.D. and Kurth, M.J., ‘Analogous’ organic synthesis of small-compound libraries: Validation of combinatorial chemistry in small-molecule synthesis, J. Am. Chem. Soc., 116 (1994) 2661–2662.

    Google Scholar 

  39. Chen, C., Ahlberg Randall, L.A., Miller, R.B., Jones, A.D. and Kurth, M.J., The solid-phase combinatorial synthesis of β-thioketones, Tetrahedron, 53 (1997) 6595–6609.

    Google Scholar 

  40. Cheng, Y. and Chapman, K.T., Solid-phase synthesis of spiroindoline, Tetrahedron Lett., 38 (1997) 1497–1500.

    Google Scholar 

  41. Cheng, B.L. and Ganesan, A., Solution-phase synthesis of α,β-amino alcohol combinatorial library, Bioorg. Med. Chem. Lett., 7 (1997) 1511–1514.

    Google Scholar 

  42. Collini, M.D. and Ellingboe, J.W., The solid-phase synthesis of trisubstituted indoles, Tetrahedron Lett., 38 (1997) 7963–7966.

    Google Scholar 

  43. Conti, P., Demont, D., Cals, J., Ottenheijm, H.C.J. and Leysen, D., A new cleavage strategy for the solid-phase synthesis of secondary amines, Tetrahedron Lett., 38 (1997) 2915–2918.

    Google Scholar 

  44. Crawshaw, M. and Hird, N.W., Synthesis of 3,4,5-trisubstituted cyclohexanones by cycloadditon to solid-phase 2-aminobutadienes, Tetrahedron Lett., 38 (1997) 7115–7118.

    Google Scholar 

  45. Cuny, G.D., Cao, J. and Hauske, J.R., Ring opening cross-metathesis on solid support, Tetrahedron Lett., 38 (1997) 5237–5240.

    Google Scholar 

  46. Dankwardt, S.M., Newman, S.R. and Krstenansky, J.L., Solid-phase synthesis of aryl and benzylpiperazines and their application in combinatorial chemistry, Tetrahedron Lett., 36 (1995) 4923–4926.

    Google Scholar 

  47. Dankwardt, S.M., Phan, T.M. and Krstenansky, J.L., Combinatorial synthesis of small-molecule libraries using 3-amino-5-hydroxybenzoic acid, Mol. Diversity, 1 (1996) 113–20.

    Google Scholar 

  48. Deshpande, M.S., Formation of carbon-carbon bond on solid support: Application of the Stille reaction, Tetrahedron Lett., 35 (1994) 5613–5614.

    Google Scholar 

  49. DeWitt, S.H., Kiely, J.S., Stankovic, C.J., Schroeder, M.C., Cody, D.M.R. and Pavia, M.R., ‘Diversomers’: An approach to nonpeptide, nonoligomeric chemical diversity, Proc. Natl. Acad. Sci. USA, 90 (1993) 6909–6913.

    Google Scholar 

  50. DeWitt, S.H. and Czarnik, A.W., Combinatorial organic synthesis using Parke-Davis's DIVERSOMER method, Acc. Chem. Res., 29 (1996) 114–122.

    Google Scholar 

  51. Dinh, T.Q. and Armstrong, R.W., Synthesis of ketones and aldehydes via reactions of Weinreb-type amides on solid support, Tetrahedron Lett., 37 (1996) 1161–1164.

    Google Scholar 

  52. Dorner, B., Husar, G.M., Ostresh, J.M. and Houghten, R.A., The synthesis of peptidomimetic combinatorial libraries through successive amide alkylations, Bioorg. Med. Chem., 4 (1996) 709–715.

    Google Scholar 

  53. Dressman, B.A., Spangle, L.A. and Kaldor, S.W., Solid-phase synthesis of hydantoins using a carbamate linker and a novel cyclization/cleavage step, Tetrahedron Lett., 37 (1996) 937–940.

    Google Scholar 

  54. Drewry, D.H., Gerritz, S.W. and Linn, J.A., Solid-phase synthesis of trisubstituted guanidines, Tetrahedron Lett., 38 (1997) 3377–3380.

    Google Scholar 

  55. Du, X. and Armstrong, R.W., Synthesis of benzofuran derivatives on solid support via SmI 2 -mediated radical cyclization, J. Org. Chem., 62 (1997) 5678–5679.

    Google Scholar 

  56. Dygutsch, D.P., Neumann, W.P. and Peterseim, M., Ring enlargement of dichloromethylcyclohexadienones via polystyrene-supported organotin hydride, Synlett., (1994) 363–365.

  57. Fagnola, M.C., Candiani, I., Visentin, G., Cabri, W., Zarini, F., Mongelli, N. and Bedeschi, A., Solid-phase synthesis of indoles using the palladium-catalysed coupling of alkynes with iodoaniline derivatives, Tetrahedron Lett., 38 (1997) 2307–2310.

    Google Scholar 

  58. Falorni, M., Giacomelli, G., Nieddu, F. and Taddei, M., A new diketopiperazine tetra-carboxylic acid as template for the homogeneous phase synthesis of chemical libraries, Tetrahedron Lett., 38 (1997) 4663–4666.

    Google Scholar 

  59. Fancelli, D., Fagnola, M.C., Severino, D. and Bedeschi, A., Solid-phase synthesis of 2-substituted benzofurans via the palladium-catalysed heteroannulation of acetylenes, Tetrahedron Lett., 38 (1997) 2311–2314.

    Google Scholar 

  60. Fathi, R., Patel, R. and Cook, A.F., Phosphorus-based combinatorial libraries: Use of amino acid derivatives as synthons, Mol. Diversity, 2 (1997) 125–134.

    Google Scholar 

  61. Fitzpatrick, L.J. and Rivero, R.A., Solid-phase synthesis of substituted aminosulfonyl ureas using a sulfonylcarbamate linker, Tetrahedron Lett., 38 (1997) 7479–7482.

    Google Scholar 

  62. Flegelova, Z. and Patek, M., Bis-allylic templates for Pd(0)-catalyzed solid-phase synthesis of tertiary amines, J. Org. Chem., 61 (1996) 6735–6738.

    Google Scholar 

  63. Fraley, M.E. and Rubino, R.S., Two methods for the preparation of 2-cyclohexenones from resin-bound 1,3-cyclohexanedione, Tetrahedron Lett., 39 (1997) 3365–3368.

    Google Scholar 

  64. Frenette, R. and Friesen, R.W., Biaryl synthesis via Suzuki coupling on a solid support, Tetrahedron Lett., 35 (1994) 9177–9180.

    Google Scholar 

  65. Furth, P.S., Reitman, M.S., Gentles, R. and Cook, A.F., Solid-phase synthesis of novel amino-ether derivatives, Tetrahedron Lett., 38 (1997) 6643–6646.

    Google Scholar 

  66. Gayo, L.M. and Suto, M.J., Ion-exchange resins for solution phase parallel synthesis of chemical libraries, Tetrahedron Lett., 38 (1997) 513–516.

    Google Scholar 

  67. Gayo, L.M. and Suto, M.J., Traceless linker: Oxidative activation and displacement of a sulfur-based linker, Tetrahedron Lett., 38 (1997) 211–214.

    Google Scholar 

  68. Goff, D.A. and Zuckermann, R.N., Solid-phase synthesis of defined 1,4-benzodiazepine-2,5-dione mixtures, J. Org. Chem., 60 (1995) 5744–5745.

    Google Scholar 

  69. Goff, D.A. and Zuckermann, R.N., Solid-phase synthesis of highly substituted peptoid 1(2 H)-isoquinolinones, J. Org. Chem., 60 (1995) 5748–5749.

    Google Scholar 

  70. Goff, D.A. and Zuckermann, R.N., The synthesis of 2-oxopiperazines by intramolecular Michael addition on solid support, Tetrahedron Lett., 37 (1996) 6247–6250.

    Google Scholar 

  71. Goodfellow, V.S., Laudeman, C.P., Gerrity, J.I., Burkard, M., Strobel, E., Zuzack, J.S. and McLeod, D.A., Rationally designed non-peptides: Variously substituted piperazine libraries for the discovery of bradykinin antagonists and other G-protein-coupled receptor ligands, Mol. Diversity, 2 (1996) 97–102.

    Google Scholar 

  72. Gopalsamy, A. and Pallai, P.V., Combinatorial synthesis of heterocycles: Solid phase synthesis of 2-arylquinoline-4-carboxylic acid derivatives, Tetrahedron Lett., 38 (1997) 907–910.

    Google Scholar 

  73. Gordeev, M.F., Patel, D.V., Wu, J. and Gordon, E.M., Approaches to combinatorial synthesis of heterocycles: Solid-phase synthesis of pyridines and pyrido[2,3-d]pyrimidines, Tetrahedron Lett., 37 (1996) 4643–4646.

    Google Scholar 

  74. Gordeev, M.F., Patel, D.V. and Gordon, E.M., Approaches to combinatorial synthesis of heterocycles: A solid-phase synthesis of 1,4-dihydropyridines, J. Org. Chem., 61 (1996) 924–928.

    Google Scholar 

  75. Gordeev, M.F., Gordon, E.M. and Patel, D.V., Solid-phase synthesis of β-sultams, J. Org. Chem., 62 (1997) 8177–8181.

    Google Scholar 

  76. Gordeev, M.F., Hui, H.C., Gordon, E.M. and Patel, D.V., A general and efficient solid phase synthesis of quinazoline-2,4-diones, Tetrahedron Lett., 38 (1997) 1729–1732.

    Google Scholar 

  77. Gordon, D.W. and Steele, J., Reductive alkylation on a solid phase: Synthesis of a piperazinedione combinatorial library, Bioorg. Med. Chem. Lett., 5 (1995) 47–50.

    Google Scholar 

  78. Gouilleux, L., Fehrentz, J.-A., Winternitz, F. and Martinez, J., Solid phase synthesis of chiral 3-substituted quinazoline-2,4-diones, Tetrahedron Lett., 37 (1996) 7031–7034.

    Google Scholar 

  79. Gowravaram, M.R. and Gallop, M.A., ‘Traceless’ solid-phase synthesis of furans via 1,3-dipolar cycloaddition reactions of isomunchnones, Tetrahedron Lett., 38 (1997) 6973–6976.

    Google Scholar 

  80. Gray, N.S., Kwon, S. and Schultz, P.G., Combinatorial synthesis of 2,9-substituted purines, Tetrahedron Lett., 38 (1997) 1161–1164.

    Google Scholar 

  81. Green,J., Solid-phase synthesis of lavendustin A and analogs, J. Org. Chem., 60 (1995) 4287–4290.

    Google Scholar 

  82. Griffith, M.C., Dooley, C.T., Houghten, R.A. and Kiely, J.S., Solid-phase synthesis, characterization, and screening of a 43 000-compound tetrahydroisoquinoline combinatorial library, In Chaiken, M. and Janda, D. (Eds) Mol. Diversity Comb. Chem.: Libr. Drug Discovery, Conf., 1996, American Chemical Society, Washington, DC, 1996, pp. 50–57.

    Google Scholar 

  83. Griffith, D.L., O'Donnell, M.J., Pottorf, R.S., Scott, W.L. and Porco, J.A.J., Tandem UPS: Sequential mono-and dialkylation of resin-bound glycine via automated synthesis, Tetrahedron Lett., 38 (1997) 8821–8824.

    Google Scholar 

  84. Guiles, J.W., Johnson, S.G. and Murray, W.V., Solid-phase Suzuki coupling for C-C bond formation, J. Org. Chem., 61 (1996) 5169–5171.

    Google Scholar 

  85. Haap, W.J., Metzger, J.W., Kempter, C. and Jung, G., Composition and purity of combinatorial aryl ether collections analyzed by electrospray mass spectrometry, Mol. Diversity, 3 (1997) 29–41.

    Google Scholar 

  86. Halm, C., Evarts, J. and Kurth, M.J., A new attachment/ cleavage strategy: Polymer-bound allylic sulfones in a solid-phase route to trisubstituted olefins, Tetrahedron Lett., 38 (1997) 7709–7712.

    Google Scholar 

  87. Hamper, B.C., Dukesherer, D.R. and South, M.S., Solid-phase synthesis of proline analogs via a three component 1,3-dipolar cycloaddition, Tetrahedron Lett., 37 (1996) 3671–3674.

    Google Scholar 

  88. Han, H., Wolfe, M.M., Brenner, S. and Janda, K.D., Liquid-phase combinatorial synthesis, Proc. Natl. Acad. Sci. USA, 92 (1995) 6419–6423.

    Google Scholar 

  89. Han, Y., Walker, S.D. and Young, R.N., Silicon directed ipso-substitution of polymer bound arylsilanes: Preparation of biaryls via the Suzuki cross-coupling reaction, Tetrahedron Lett., 37 (1996) 2703–2706.

    Google Scholar 

  90. Hanessian, S. and Yang, R.-Y., Solution and solid phase synthesis of 5-alkoxyhydantoin libraries with a three-fold functional diversity, Tetrahedron Lett., 37 (1996) 5835–5838.

    Google Scholar 

  91. Harriman, G.C.B., Synthesis of small and medium sized 2,2-disubstituted lactams via the ‘intramolecular’ three component Ugi reaction, Tetrahedron Lett., 38 (1997) 5591–5594.

    Google Scholar 

  92. Heinonen, P. and Lonnberg, H., A novel solid support for derivatization and subsequent N-alkylation of secondary amines: Preparation of N-alkylated 5-and 6-alkoxy-1,2,3,4-tetrahydroisoquinolines via Mitsunobu reaction, Tetrahedron Lett., 38 (1997) 8569–8572.

    Google Scholar 

  93. Heizmann, G. and Eberle, A.N., Xanthines as a scaffold for molecular diversity, Mol. Diversity, 2 (1997) 171–174.

    Google Scholar 

  94. Hird, N.W., Solid-phase synthesis of 2-aminobutadienes using a piperazine linker, Tetrahedron Lett., 38 (1997) 7111–7114.

    Google Scholar 

  95. Hiroshige, M., Hauske, J.R. and Zhou, P., Formation of CC bond in solid phase synthesis using the Heck reaction, Tetrahedron Lett., 36 (1995) 4567–4570.

    Google Scholar 

  96. Hiroshige, M., Hauske, J.R. and Zhou, P., Palladium-mediated macrocyclization on solid support and its applications to combinatorial synthesis, J. Am. Chem. Soc., 117 (1995) 11590–11591.

    Google Scholar 

  97. Ho, C.Y. and Kukla, M.J., Carbamate linkers as latent N-methylamines in solid phase synthesis, Tetrahedron Lett., 38 (1997) 2799–2802.

    Google Scholar 

  98. Hollinshead, S.P., Stereoselective synthesis of highly functionalized pyrrolidines via 1,3-dipolar cycloaddition reactions on a solid support, Tetrahedron Lett., 37 (1996) 9157–9160.

    Google Scholar 

  99. Holmes, C.P., Chinn, J.P., Look, G.C., Gordon, E.M. and Gallop, M.A., Strategies for combinatorial organic synthesis: Solution and polymer-supported synthesis of 4-thiazolidinones and 4-metathiazanones derived from amino acids, J. Org. Chem., 60 (1995) 7328–7333.

    Google Scholar 

  100. Hutchines, S.M. and Chapman, K.T., Solid phase synthesis of tetrahydroisoquinolines and tetrahydroimidazopyridines, Tetrahedron Lett., 37 (1996) 4865–4868.

    Google Scholar 

  101. Hutchins, S.M. and Chapman, K.T., A general method for the solid phase syntheis of ureas, Tetrahedron Lett., 35 (1994) 4055–4058.

    Google Scholar 

  102. Hutchins, S.M. and Chapman, K.T., A strategy for urea linked diamine libraries, Tetrahedron Lett., 36 (1995) 2583–2586.

    Google Scholar 

  103. Hutchins, S.M. and Chapman, K.T., Fischer indole synthesis on a solid support, Tetrahedron Lett., 37 (1996) 4869–4872.

    Google Scholar 

  104. Johnson, C.R. and Zhang, B., Solid phase synthesis of alkenes using the Horner-Wadsworth-Emmons reaction and monitoring by gel phase 31 P NMR, Tetrahedron Lett., 36 (1995) 9253–9256.

    Google Scholar 

  105. Kaljuste, K. and Unden, A., Solid-phase synthesis of 1,2,3,4-tetrahydro-β-carbolines. Implications for combinatorial chemistry, Tetrahedron Lett., 36 (1995) 9211–9214.

    Google Scholar 

  106. Katritzky, A.R., Xie, L. and Zhang, G., Synthesis of primary amines via nucleophilic addition of organometallic reagents to aldimines on solid support, Tetrahedron Lett., 38 (1997) 7011–7014.

    Google Scholar 

  107. Kay, C., Murray, P.J., Sandow, L. and Holmes, A.B., A novel, chemically robust, amine releasing linker, Tetrahedron Lett., 38 (1997) 6941–6944.

    Google Scholar 

  108. Keating, T.A. and Armstrong, R.W., Molecular diversity via a convertible isocyanide in the Ugi four-component condensation, J. Am. Chem. Soc., 117 (1995) 7842–7843.

    Google Scholar 

  109. Keating, T.A. and Armstrong, R.W., A remarkable two-step synthesis of diverse 1,4-benzodiazepine-2,5-diones using the Ugi four-component condensation, J. Org. Chem., 61 (1996) 8935–8939.

    Google Scholar 

  110. Keating, T.A. and Armstrong, R.W., Postcondensation modifications of Ugi four-component condensation products: 1-Isocyanocyclohexene as a convertible isocyanide. Mechanism of conversion, synthesis of diverse structures, and demonstration of resin capture, J. Am. Chem. Soc., 118 (1996) 2574–2583.

    Google Scholar 

  111. Khan, N.M., Arumugam, V. and Balasubramanian, S., Solid-phase reductive alkylation of secondary amines, Tetrahedron Lett., 37 (1996) 4819–4822.

    Google Scholar 

  112. Khound, S. and Das, P.J., Solid-phase synthesis of N-arylazoindoles, Tetrahedron, 53 (1997) 9749–9754.

    Google Scholar 

  113. Kim, J.-M., Bi, Y., Paikoff, S.J. and Schultz, P.G., The solid-phase synthesis of oligoureas, Tetrahedron Lett., 37 (1996) 5305–5308.

    Google Scholar 

  114. Kim, S.W., Ahn, S.Y., Koh, J.S., Lee, J.H., Ro, S. and Cho, H.Y., Solid-phase synthesis of hydantoin libraries using a novel cyclization and traceless cleavage step, Tetrahedron Lett., 38 (1997) 4603–4606.

    Google Scholar 

  115. Kiselyov, A.S. and Armstrong, R.W., Solid support synthesis of tetrahydroquinolines via the Grieco three component condensation, Tetrahedron Lett., 38 (1997) 6163–6166.

    Google Scholar 

  116. Kobayashi, S. and Nagayama, S., A new methodology for combinatorial synthesis. Preparation of diverse quinoline derivatives using a novel polymer-supported scandium catalyst, J. Am. Chem. Soc., 118 (1996) 8977–8978.

    Google Scholar 

  117. Kobayashi, S., Hachiya, I., Syzuki, S. and Moriwaki, M., Polymer-supported silyl enol ethers. Synthesis and reactions with imines for the preparation of an amino alcohol library, Tetrahedron Lett., 37 (1996) 2809–2812.

    Google Scholar 

  118. Kobayashi, S., Moriwaki, M., Akiyama, R., Suzuki, S. and Hachiya, I., Parallel synthesis using Mannich-type three-component reactions and ‘field synthesis’ for the construction of an amino alcohol library, Tetrahedron Lett., 37 (1996) 7783–7786.

    Google Scholar 

  119. Kobayashi, S., Hachiya, I. and Yasuda, M., Aldol reactions on solid-phase. Sc(OTf) 3 -catalyzed Aldol reactions of polymer-supported silyl enol ethers with aldehydes providing convenient methods for the preparation of 1,3-diol, α-hydroxy carboxylic acid, and α-hydroxy aldehyde libraries, Tetrahedron Lett., 37 (1996) 5569–5572.

    Google Scholar 

  120. Kocis, P., Issakova, O., Sepetov, N.F. and Lebl, M., Kemp's triacid scaffolding for synthesis of combinatorial nonpeptide uncoded libraries, Tetrahedron Lett., 36 (1995) 6623–6626.

    Google Scholar 

  121. Koh, J.S. and Ellman, J.A., Palladium-mediated three-component coupling strategy for the solid-phase synthesis of tropane derivatives, J. Org. Chem., 61 (1996) 4494–4495.

    Google Scholar 

  122. Kolodziej, S.A. and Hamper, B.C., Solid-phase synthesis of 5,6-dihydropyrimidine-2,4-diones, Tetrahedron Lett., 37 (1996) 5277–5280.

    Google Scholar 

  123. Krchnak, V., Flegelova, Z., Weichsel, A.S. and Lebl, M., Polymer-supported Mitsunobu ether formation and its use in combinatorial chemistry, Tetrahedron Lett., 36 (1995) 6193–6196.

    Google Scholar 

  124. Krchnak, V., Weichsel, A.S., Cabel, D., Flegelova, Z. and Lebl, M., Structurally homogeneous and heterogeneous synthetic combinatorial libraries, Mol. Diversity, 1 (1996) 149–164.

    Google Scholar 

  125. Krchnak, V., Weichsel, A.S., Issakova, O., Lam, K.S. and Lebl, M., Bifunctional scaffolds as templates for synthetic combinatorial libraries, Mol. Diversity, 1 (1996) 177–182.

    Google Scholar 

  126. Krchnak, V. and Weichsel, A.S., Polymer-supported synthesis of diverse perhydro-1,4-diazepine-2,5-diones, Tetrahedron Lett., 38 (1997) 7299–7302.

    Google Scholar 

  127. Kurth, M.J., Randall, L.A.A., Chen, C., Melander, C. and Miller, R.B., Library-based lead compound discovery: Antioxidants by an analogous synthesis/deconvolutive assay strategy, J. Org. Chem., 59 (1994) 5862–5864.

    Google Scholar 

  128. Kurth, M.J., Randall, L.A.A. and Takenouchi, K., Solid-phase combinatorial synthesis of polyisoxazolines: A two-reaction iterative protocol, J. Org. Chem., 61 (1996) 8755–8761.

    Google Scholar 

  129. Lawrence, R.M., Biller, S.A., Fryszman, O.M. and Poss, M.A., Automated synthesis and purification of amides. Exploitation of automated solid-phase extraction in organic synthesis, Synthesis, (1997) 553–558.

  130. Le Hetet, C., David, M., Carreaux, F., Carbni, B. and Sauleau, A., Synthesis of functionalized γ and δ-lactones via polymer-bound epoxides, Tetrahedron Lett., 38 (1997) 5153–5156.

    Google Scholar 

  131. Lee, J., Murray, W.V. and Rivero, R.A., Solid-phase synthesis of 3,4-disubstituted-7-carbamoyl-1,2,3,4-tetrahydroquinoxalin-2-ones, J. Org. Chem., 62 (1997) 3874–3879.

    Google Scholar 

  132. Ley, S.V., Mynett, D.M. and Koot, W.-J., Solid phase synthesis of bicyclo[2.2.2]octane derivatives via tandem Michael addition reactions and subsequent reductive amination, Synlett., (1995) 1017–1020.

  133. Liang, R., Yan, L., Loebach, J., Ge, M., Uozumi, Y., Sekanina, K., Horan, N., Gildersleeve, J., Thompson, C., Smith, A., Biswas, K., Still, W.C. and Kahne, D., Parallel synthesis and screening of a solid phase carbohydrate library, Science, 274 (1996) 1520–1522.

    Google Scholar 

  134. Lorsbach, B.A., Miller, R.B. and Kurth, M.J., Reissert-based ‘traceless’ solid-phase synthesis: Isoquinoline, and isoxazoline-containing heterocycles, J. Org. Chem., 61 (1996) 8716–8717.

    Google Scholar 

  135. MacDonald, A.A., DeWitt, S.H., Hogan, E.M. and Ramage, R., A solid phase approach to quinolones using the DIVERSOMER technology, Tetrahedron Lett., 37 (1996) 4815–4818.

    Google Scholar 

  136. Marquais, S. and Arlt, M., Aryl-aryl cross coupling on a solid support using zinc organic reagents and palladium catalysis, Tetrahedron Lett., 37 (1996) 5491–5494.

    Google Scholar 

  137. Marsh, I.R., Smith, H.K., Leblanc, C. and Bradley, M., Synthetic methods for polyamine linkers and their application to combinatorial chemistry, Mol. Diversity, 2 (1997) 165–170.

    Google Scholar 

  138. Marti, R.E., Bleicher, K.H. and Bair, K.W., Solid phase synthesis of β-peptides via Arndt-Eistert homologation of Fmoc-protected amino acid diazoketones, Tetrahedron Lett., 38 (1997) 6145–6148.

    Google Scholar 

  139. Marx, M.A., Grillot, A.-L., Louer, C.T., Beaver, K.A. and Bartlett, P.A., Synthetic design for combinatorial chemistry. Solution and polymer-supported synthesis of polycyclic lactams by intramolecular cyclization of azomethine ylides, J. Am. Chem. Soc., 119 (1997) 6153–6167.

    Google Scholar 

  140. Marzinzik, A.L. and Felder, E.R., Solid support synthesis of highly functionalized pyrazoles and isoxazoles, scaffolds for molecular diversity, Tetrahedron Lett., 37 (1996) 1003–1006.

    Google Scholar 

  141. Mayer, J.P., Bankaitis-Davis, D., Zhang, J., Beaton, G., Bjergarde, K., Andersen, C.M., Goodman, B.A. and Herrera, C.J., Application of the Pictet-Spengler reaction in combinatorial chemistry, Tetrahedron Lett., 37 (1996) 5633–5636.

    Google Scholar 

  142. Mayer, J.P., Zhang, J., Bjergarde, K., Lenz, D.M. and Gaudino, J.J., Solid-phase synthesis of 1,4-benzodiazepine-2,5-diones, Tetrahedron Lett., 37 (1996) 8081–8084.

    Google Scholar 

  143. Mayer, J.P., Lewis, G.S., Curtis, M.J. and Zhang, J., Solid phase synthesis of quinazolinones, Tetrahedron Lett., 38 (1997) 8445–8448.

    Google Scholar 

  144. Meutermans, W.D.F. and Alewood, P.F., The solid-phase synthesis of dihydro-and tetrahydroisoquinolines, Tetrahedron Lett., 36 (1995) 7709–7712.

    Google Scholar 

  145. Meyers, H.V., Dilley, G.J., Durgin, T.L., Powers, T.S., Winssinger, N.A., Zhu, H. and Pavia, M.R., Multiple simultaneous synthesis of phenolic libraries, Mol. Diversity, 1 (1995) 13–20.

    Google Scholar 

  146. Mjalli, A.M.M., Sarshar, S. and Baiga, T.J., Solid-phase synthesis of pyrroles derived from a four component condensation, Tetrahedron Lett., 37 (1996) 2943–2946.

    Google Scholar 

  147. Mohan, R., Chou, Y.-L. and Morrissey, M.M., Pictet-Spengler reaction of solid support: Synthesis of 1,2,3,4-tetrahydro-β-carboline libraries, Tetrahedron Lett., 37 (1996) 3963–3966.

    Google Scholar 

  148. Moroder, L., Lutz, J., Grams, F. and Rudolph-Bohner, S., A new efficient method for the synthesis of 1,4-benzodiazepine-2,5-dione diversomers, Biopolymers, 38 (1996) 295–300.

    Google Scholar 

  149. Nefzi, A., Ostresh, J.M., Meyer, J.-P. and Houghten, R.A., Solid-phase synthesis of heterocyclic compounds from linear peptides: Cyclic ureas and thioureas, Tetrahedron Lett., 38 (1997) 931–934.

    Google Scholar 

  150. Nefzi, A., Ostresh, J.M. and Houghten, R.A., Solid-phase synthesis of 1,3,4,7-tetrasubstituted perhydro-1,4-diazepine-2,5-diones, Tetrahedron Lett., 38 (1997) 4943–4946.

    Google Scholar 

  151. Neuville, L. and Zhu, Z., Solution phase combinatorial synthesis of arylpiperazines, Tetrahedron Lett., 38 (1997) 4091–4094.

    Google Scholar 

  152. Ngu, K. and Patel, D.V., A new and efficient solid-phase synthesis of hydroxamic acids, J. Org. Chem., 62 (1997) 7088–7089.

    Google Scholar 

  153. Nielsen, J. and Lyngsoe, L.O., Combinatorial solid-phase synthesis of balanol analogs, Tetrahedron Lett., 37 (1996) 8439–8442.

    Google Scholar 

  154. Nielsen, J. and Rasmussen, P.H., Implementation of a combinatorial cleavage and deprotection scheme. 1. Synthesis of phthalhydrazide libraries, Tetrahedron Lett., 37 (1996) 3351–3354.

    Google Scholar 

  155. Nielsen, J. and Jensen, F.R., Solid-phase synthesis of small molecule libraries using double combinatorial chemistry, Tetrahedron Lett., 38 (1997) 2011–2014.

    Google Scholar 

  156. Nugiel, D.A., Cornelius, L.A.M. and Corbett, J.W., Facile preparation of 2,6-disubstituted purines using solid-phase chemistry, J. Org. Chem., 62 (1997) 201–203.

    Google Scholar 

  157. Obrecht, D., Abrecht, C., Grieder, A. and Villalgordo, J.M., A novel and efficient approach for the combinatorial synthesis of structurally diverse pyrimidines on solid support, Helv. Chim. Acta, 80 (1997) 65–72.

    Google Scholar 

  158. Panek, J.S. and Zhu, B., Synthesis of aromatic 1,2-diazines by inverse electron demand Diels-Alder reaction of polymer-supported 1,2,4,5-tetrazines, Tetrahedron Lett., 37 (1996) 8151–8154.

    Google Scholar 

  159. Panek, J.S. and Zhu, B., Asymmetric crotylation reaction on solid support: Synthesis of stereochemically well-defined polypropionate-like subunits, J. Am. Chem. Soc., 119 (1997) 12022–12023.

    Google Scholar 

  160. Parlow, J.J., The use of anion exchange resins for the synthesis of combinatorial libraries containing aryl and heteroaryl ethers, Tetrahedron Lett., 37 (1996) 5257–5260.

    Google Scholar 

  161. Parlow, J.J., Mischke, D.A. and Woodard, S.S., Utility of complementary molecular reactivity and molecular recognition (CMR/R) technology and polymer-supported reagents in the solution-phase synthesis of heterocyclic carboxamides, J. Org. Chem., 62 (1997) 5908–5919.

    Google Scholar 

  162. Patek, M., Drake, B. and Lebl, M., All-cis cyclopentane scaffolding for combinatorial solid-phase synthesis of small non-peptide compounds, Tetrahedron Lett., 35 (1994) 9169–9172.

    Google Scholar 

  163. Patek, M., Drake, B. and Lebl, M., Solid-phase synthesis of ‘small’ organic molecules based on thiazolidine scaffold, Tetrahedron Lett., 36 (1995) 2227–2230.

    Google Scholar 

  164. Pavia, M.R., Cohen, M.P., Dilley, G.J., Dubuc, G.R., Durgin, T.L., Forman, F.W., Hediger, M. E., Milot, G., Powers, T.S., Sucholeiki, I., Zhou, S. and Hangauer, D.G., The design and synthesis of substituted biphenyl libraries, Bioorg. Med. Chem., 4 (1996) 659–666.

    Google Scholar 

  165. Pearson, W.H. and Clark, R.B., Solid-phase synthesis of pyrrolidines via 2-azaallyl anion cycloadditions with alkenes, Tetrahedron Lett., 38 (1997) 7669–7672.

    Google Scholar 

  166. Pei, Y. and Moos, W.H., Post-modification of peptoid side chains: [3+2] cycloaddition of nitrile oxides with alkenes and alkynes on the solid-phase, Tetrahedron Lett., 35 (1994) 5825–5828.

    Google Scholar 

  167. Pei, Y., Houghten, R.A. and Kiely, J.S., Synthesis of 4-amino-3,4-dihydro-2(1H)-quinolinones via β-lactam intermediates on a solid-phase, Tetrahedron Lett., 38 (1997) 3349–3352.

    Google Scholar 

  168. Phillips, G.B. and Ping, W.G., Solid-phase synthesis of benzimidazoles, Tetrahedron Lett., 37 (1996) 4887–4890.

    Google Scholar 

  169. Piettre, S.R. and Baltzer, S., A new approach to the solid-phase Suzuki coupling reaction, Tetrahedron Lett., 38 (1997) 1197–1200.

    Google Scholar 

  170. Pitlik, J. and Townsend, C.A., Solution-phase synthesis of a combinatorial monocyclic β-lactam library: Potential protease inhibitors, Bioorg. Med. Chem. Lett., 7 (1997) 3129–3134.

    Google Scholar 

  171. Plunkett, M.J. and Ellman, J.A., A silicon-based linker for traceless solid-phase synthesis, J. Org. Chem., 60 (1995) 6006–6007.

    Google Scholar 

  172. Plunkett, M.J. and Ellman, J.A., Solid-phase synthesis of structurally diverse 1,4-benzodiazepine derivatives using the Stille coupling reaction, J. Am. Chem. Soc., 117 (1995) 3306–3307.

    Google Scholar 

  173. Plunkett, M.J. and Ellman, J.A., Germanium and silicon linking strategies for traceless solid-phase synthesis, J. Org. Chem., 62 (1997) 2885–2893.

    Google Scholar 

  174. Pothion, C., Fehrentz, J.-A., Aumelas, A., Loffet, A. and Martinez, J., Synthesis of pyrrolidine-2,4-diones from urethane N-carboxyanhydrides (UNCAs), Tetrahedron Lett., 37 (1996) 1027–1030.

    Google Scholar 

  175. Prien, O., Rolfing, K., Thiel, M. and Kunzer, H., Combinatorial synthesis of C(2), C(3)-disubstituted 3-hydroxypropionamides utilizing Baylis-Hillman reactions on solid support, Synlett., (1997) 325–326.

  176. Raju, B. and Kogan, T.P., Solid-phase synthesis of sulfonamides using a carbamate linker, Tetrahedron Lett., 38 (1997) 3373–3376.

    Google Scholar 

  177. Rano, T.A. and Chapman, K.T., Solid-phase synthesis of aryl ethers via the Mitsunobu reaction, Tetrahedron Lett., 36 (1995) 3789–3792.

    Google Scholar 

  178. Robinson, S. and Roskamp, E.J., Solid-phase synthesis of guanidines, Tetrahedron, 53 (1997) 6697–6705.

    Google Scholar 

  179. Roelfing, K., Thiel, M. and Kuenzer, H., 1,2,6-Trisubstituted tetrahydroisoquinoline derivatives by solid-phase synthesis, Synlett., (1996) 1036–1038.

  180. Rossen, K., Sager, J. and DiMichele, L.M., An efficient and versatile synthesis of piperazine-2-carboxamides, Tetrahedron Lett., 38 (1997) 3183–3186.

    Google Scholar 

  181. Rottlander, M. and Knochel, P., Multiple cross-coupling reactions of aryl and benzylic zinc halides with aryl halides and triflates in solid-phase synthesis of polyfunctional aromatics, Synlett., (1997) 1084–1086.

  182. Routledge, A., Abell, C. and Balasubramanian, S., An investigation into solid-phase radical chemistry – synthesis of furan rings, Synlett., (1997) 61–62.

  183. Ruhland, B., Bhandari, A., Gordon, E.M. and Gallop, M.A., Solid-supported combinatorial synthesis of structurally diverse β-lactams, J. Am. Chem. Soc., 118 (1996) 253–254.

    Google Scholar 

  184. Ruhland, T. and Kunzer, H., Structurally diverse 2,6-disubstituted quinoline derivatives by solid-phase synthesis, Tetrahedron Lett., 37 (1996) 2757–2760.

    Google Scholar 

  185. Ruhland, B., Bromrun, A. and Gallop, M.A., Solid-phase synthesis of 4-arylazetidin-2-ones via Suzuki and Heck cross-coupling reactions, J. Org. Chem., 62 (1997) 7820–7826.

    Google Scholar 

  186. Sarshar, S., Siev, D. and Mjalli, A.M.M., Imidazole libraries on solid support, Tetrahedron Lett., 37 (1996) 835–838.

    Google Scholar 

  187. Schuster, M., Lucas, N. and Blechert, S., Ruthenium-catalyzed cross metathesis binding of functionalized olefins to polystyrene resin via a novel allylsilyl linker suitable for electrophilic cleavage, J. Chem. Soc., Chem. Commun., (1997) 823–824.

  188. Scialdone, M.A., Diisocyanates as scaffolds for combinatorial libraries. The solid-phase synthesis of bis ureas from polymer-supported diisocyanates, Tetrahedron Lett., 37 (1996) 8141–8144.

    Google Scholar 

  189. Scott, B.O., Siegmund, A.C., Marlowe, C.K., Pei, Y. and Spear, K.L., Solid phase organic synthesis (SPOS): A novel route to diketopiperazines and diketomorpholines, Mol. Diversity, 1 (1995) 125–134.

    Google Scholar 

  190. Short, K.M., Ching, B.W. and Mjalli, A.M.M., The synthesis of hydantoin 4-imides on solid support, Tetrahedron Lett., 37 (1996) 7489–7492.

    Google Scholar 

  191. Short, K.M., Ching, B.W. and Mjalli, A.M.M., Exploitation of the Ugi 4CC reaction: Preparation of small molecule combinatorial libraries via solid phase, Tetrahedron, 53 (1997) 6653–6679.

    Google Scholar 

  192. Shuker, A.J., Siegel, M.G., Matthews, D.P. and Weigel, L.O., The application of high-throughput synthesis and purification to the preparation of ethanolamines, Tetrahedron Lett., 38 (1997) 6149–6152.

    Google Scholar 

  193. Sibi, M.P. and Chandramouli, S.V., Intermolecular free radical reactions on solid support. Allylation of esters, Tetrahedron Lett., 38 (1997) 8929–8932.

    Google Scholar 

  194. Sim, M.M. and Ganesan, A., Solution-phase synthesis of a combinatorial thiohydantoin library, J. Org. Chem., 62 (1997) 3230–3235.

    Google Scholar 

  195. Sim, M.M., Lee, C.L. and Ganesan, A., Combinatorial synthesis of 2-thioxo-4-dihydropyrimidinones, J. Org. Chem., 62 (1997) 9358–9360.

    Google Scholar 

  196. Smith, J., Liras, J.L., Schneider, S.E. and Anslyn, E.V., Solid and solution phase organic syntheses of oligomeric thioureas, J. Org. Chem., 61 (1996) 8811–8818.

    Google Scholar 

  197. Smith, A.L., Thomson, C.G. and Leeson, P.D., An efficient solid-phase synthetic route to 1,3-disubstituted (1 H,3 H)-quinazoline-2,4-diones suitable for combinatorial synthesis, Bioorg. Med. Chem. Lett., 6 (1996) 1483–1486.

    Google Scholar 

  198. Spitzer, J.L., Kurth, M.J. and Schore, N.E., Polymer-supported synthesis as a tool for improving chemoselectivity: Pauson-Khand reaction, Tetrahedron, 53 (1997) 6791–6808.

    Google Scholar 

  199. Stankova, M. and Lebl, M., Library generation through successive substitution of trichlorotriazine, Mol. Diversity, 2 (1996) 75–80.

    Google Scholar 

  200. Stephensen, H. and Zaragoza, F., Resin-bound isothiocyanates and their synthetic equivalents as intermediates for the solid-phase synthesis of substituted thiophenes, J. Org. Chem., 62 (1997) 6090–6097.

    Google Scholar 

  201. Strocker, A.M., Keating, T.A., Tempest, P.A. and Armstrong, R.W., Use of a convertible isocyanide for generation of Ugi derivatives on solid support: Synthesis of α-acylaminoesters and pyrroles, Tetrahedron Lett., 37 (1996) 1149–1152.

    Google Scholar 

  202. Sutherlin, D.P., Stark, T.M., Hughes, R. and Armstrong, R.W., Generation of C-glycoside peptide ligands for cell surface carbohydrate receptors using a four-component condensation on solid support, J. Org. Chem., 61 (1996) 8350–8354.

    Google Scholar 

  203. Szardenings, A.K., Burkoth, T.S., Lu, H.H., Tien, D.W. and Campbell, D.A., A simple procedure for the solid phase synthesis of diketopiperazine and diketomorpholine derivatives, Tetrahedron, 53 (1997) 6573–6593.

    Google Scholar 

  204. Tempest, P.A., Brown, S.D. and Armstrong, R.W., Solid-phase, parallel syntheses by Ugi multicomponent condensation, Angew. Chem. Int. Ed. Engl., 35 (1996) 640–642.

    Google Scholar 

  205. Tempest, P.A. and Armstrong, R.W., Cyclobutenedione derivatives on solid support: Toward multiple core structure libraries, J. Am. Chem. Soc., 119 (1997) 7607–7608.

    Google Scholar 

  206. Thomas, J.B., Fall, M.J., Cooper, J.B., Burgess, J.P. and Carroll, F.I., Rapid in-plate generation of benzimidazole libraries and amide formation using EEDQ, Tetrahedron Lett., 38 (1997) 5099–5102.

    Google Scholar 

  207. Tietze,L.F. and Steinmetz, A., A general and expedient method for the solid-phase synthesis of structurally diverse 1-phenyl-pyrazolone derivatives, Synlett., (1996) 667–668.

  208. Tietze, L.F., Hippe, T. and Steinmetz, A., Solid-phase three-component domino reactions. Combinatorial approach to substituted 3,4-dihydro-2 H-pyrans, Synlett., (1996) 1043–1044.

  209. Tietze, L.F. and Steinmetz, A., Stereoselective solid-phase synthesis of cyclopentane and cyclohexane derivatives by two-component domino reactions: Generation of combinatorial libraries, Angew. Chem. Int. Ed. Engl., 35 (1996) 651–652.

    Google Scholar 

  210. Tietze, L.F., Steinmetz, A. and Balkenhohl, F., Solid-phase synthesis of polymer-bound β-ketoesters and their application in the synthesis of structurally diverse pyrazolones, Bioorg. Med. Chem. Lett., 7 (1997) 1303–1306.

    Google Scholar 

  211. Tortolani, D.R. and Biller, S.A., A solid-phase synthesis of miconazole analogs via an iodoetherification reaction, Tetrahedron Lett., 37 (1996) 5687–5690.

    Google Scholar 

  212. Ugi, I., Goebel, M., Gruber, B., Heilingbrunner, M., Heiss, B., Hoerl, W., Kern, O. and Starnecker, M., Molecular libraries in liquid phase via Ugi-MCR, Res. Chem. Intermed., 22 (1996) 625–644.

    Google Scholar 

  213. van Maarseveen, J.H., den Hartog, J.A.J., Engelen, V., Finner, E., Visser, G. and Kruse, C.G., Solid phase ring-closing metathesis: Cyclization/cleavage approach towards a seven membered cycloolefin, Tetrahedron Lett., 37 (1996) 8249–8252.

    Google Scholar 

  214. Virgilio, A.A. and Ellman, J.A., Simultaneous solid-phase synthesis of β-turn mimetics incorporating side-chain functionality, J. Am. Chem. Soc., 116 (1994) 11580–11581.

    Google Scholar 

  215. Virgilio, A.A., Schurer, S.C. and Ellman, J.A., Expedient solid-phase synthesis of putative β-turn mimetics incorporating the i+1, i+2, and i+3 sidechains, Tetrahedron Lett., 37 (1996) 6961–6964.

    Google Scholar 

  216. Vo, N.H., Eyermann, C.J. and Hodge, C.N., Transformations of resin-bound pyridinium ylides: I. A stereoselective synthesis of 2,2,3-trisubstituted cyclopropanecarboxylates, Tetrahedron Lett., 38 (1997) 7951–7954.

    Google Scholar 

  217. Wallace, O.B., Solid-phase synthesis of ketones from esters, Tetrahedron Lett., 38 (1997) 4939–4942.

    Google Scholar 

  218. Wang, G.T., Chen, Y., Wang, S., Sciotti, R. and Sowin, T., Solid-phase synthesis of ureas of secondary amines via carbamoyl chloride, Tetrahedron Lett., 38 (1997) 1895–1898.

    Google Scholar 

  219. Wang, F. and Hauske, J.R., Solid-phase synthesis of benzoxazoles via Mitsunobu reaction, Tetrahedron Lett., 38 (1997) 6529–6532.

    Google Scholar 

  220. Wang, F. and Hauske, J.R., Solid-phase synthesis of 3,4-dihydroquinazoline, Tetrahedron Lett., 38 (1997) 8651–8654.

    Google Scholar 

  221. Wang, Y. and Wilson, S.R., Solid-phase synthesis of 2,3-dihydro-4-pyridones: Reaction of Danishefsky's diene with polymer-bound imines, Tetrahedron Lett., 38 (1997) 4021–4024.

    Google Scholar 

  222. Ward, Y.D. and Farina, V., Solid-phase synthesis of aryl amines via palladium catalyzed amination of resin-bound aromatic bromides, Tetrahedron Lett., 37 (1996) 6993–6996.

    Google Scholar 

  223. Watson, S.R., Wilson, R.D., Judd, D.B. and Richards, S.A., Solid-phase synthesis of 5-aminopyrazoles and derivatives, Tetrahedron Lett., 38 (1997) 9065–9068.

    Google Scholar 

  224. Willoughby, C.A. and Chapman, K.T., Solid-phase synthesis of aryl amines, Tetrahedron Lett., 37 (1996) 7181–7184.

    Google Scholar 

  225. Wipf, P. and Cunningham, A., A solid phase protocol of the Biginelli dihydropyrimidine synthesis suitable for combinatorial chemistry, Tetrahedron Lett., 36 (1995) 7819–7822.

    Google Scholar 

  226. Wipf, P. and Henninger, T.C., Solid-phase synthesis of peptide mimetics with (E)-alkene amide bond replacements derived from alkenylaziridines, J. Org. Chem., 62 (1997) 1586–1587.

    Google Scholar 

  227. Wipf, P. and Venkatraman, S., An improved protocol for azole synthesis with PEG-supported Burgess reagent, Tetrahedron Lett., 37 (1996) 4659–4662.

    Google Scholar 

  228. Woolard, F.X., Paetsch, J. and Ellman, J.A., A silicon linker for direct loading of aromatic compounds to supports. Traceless synthesis of pyridine-based tricyclics, J. Org. Chem., 62 (1997) 6102–6103.

    Google Scholar 

  229. Wuonola, M.A. and Powers, D.G., Use of combinatorial libraries in the discovery and development of novel anti-infectives, In Chaiken, I.M. and Janda, K.D. (Eds) Mol. Diversity Comb. Chem.: Libr. Drug Discovery, Conf., 1996, American Chemical Society, Washington, DC, 1996, pp. 284–297.

    Google Scholar 

  230. Xiao, X.-Y., Parandoosh, Z. and Nova, M.P., Design and synthesis of a taxoid library using radiofrequency encoded combinatorial chemistry, J. Org. Chem., 62 (1997) 6029–6033.

    Google Scholar 

  231. Xiao, X.-Y., Ngu, K., Chao, C. and Patel, D.V., Selective solid phase synthesis of ureas and hydantoins from common phenyl carbamate intermediates, J. Org. Chem., 62 (1997) 6968–6973.

    Google Scholar 

  232. Xu, W., Mohan, R. and Morrissey, M.M., Polymer-supported bases in combinatorial chemistry: Synthesis of aryl ethers from phenols and alkyl halides and aryl halides, Tetrahedron Lett., 38 (1997) 7337–7340.

    Google Scholar 

  233. Yan, B. and Gstach, H., An indazole synthesis on solid support monitored by single bead FTIR microspectroscopy, Tetrahedron Lett., 37 (1996) 8325–8328.

    Google Scholar 

  234. Yang, L. and Guo, L., Pictet-Spengler reaction on solid support, Tetrahedron Lett., 37 (1996) 5041–5044.

    Google Scholar 

  235. Yoo, S.-E., Seo, J.-S., Yi, K.-Y. and Gong, Y.-D., Solid-phase synthesis of biphenyltetrazole derivatives, Tetrahedron Lett., 38 (1997) 1203–1206.

    Google Scholar 

  236. Youngman, M.A. and Dax, S.L., Mannich reactions of a resin-bound terminal alkyne, Tetrahedron Lett., 38 (1997) 6347–6350.

    Google Scholar 

  237. Yu, K.-L., Deshpande, M.S. and Vyas, D.M., Heck reactions in solid-phase synthesis, Tetrahedron Lett., 35 (1994) 8919–22.

    Google Scholar 

  238. Yun, W. and Mohan, R., Heck reaction on solid support: Synthesis of indole analogs, Tetrahedron Lett., 37 (1996) 7189–7192.

    Google Scholar 

  239. Zaragoza, F., Carbon-carbon bond formation on solid support: Synthesis of monoacyl piperazines by Knoevenageltype condensation reactions, Tetrahedron Lett., 36 (1995) 8677–8678.

    Google Scholar 

  240. Zaragoza, F., Solid-phase synthesis of substituted 3-aminothiophenes and 2-methylene-2,3-dihydrothiazoles, Tetrahedron Lett., 37 (1996) 6213–6216.

    Google Scholar 

  241. Zaragoza, F. and Petersen, S.V., Solid-phase synthesis of substitued 1,2,3-triazoles, Tetrahedron, 52 (1996) 10823–10826.

    Google Scholar 

  242. Zaragoza, F. and Petersen, S.V., Generation of rhodium carbenoids on a polystyrene support and their OH-insertion reaction with alcohols, Tetrahedron, 52 (1996) 5999–6002.

    Google Scholar 

  243. Zaragoza, F., Solid-phase synthesis of cyanoacetamidines: Fast access to potential bioisosteres of acceptor-substituted guanidines, Tetrahedron Lett., 38 (1997) 7291–7294.

    Google Scholar 

  244. Zhang, C., Moran, E.J., Woiwode, T.F., Short, K.M. and Mjalli, A.M.M., Synthesis of tetrasubstituted imidazoles via α-(N-acyl-N-alkylamino)-β-ketoamides on Wang resin, Tetrahedron Lett., 37 (1996) 751–754.

    Google Scholar 

  245. Zhang, C. and Mjalli, A.M.M., A combinatorial method for the solid-phase synthesis of α-amino phosphonates and phosphonic acids, Tetrahedron Lett., 37 (1996) 5457–5460.

    Google Scholar 

  246. Zhang, H.-C. and Maryanoff, B.E., Construction of indole and benzofuran systems on the solid-phase via palladium-mediated cyclizations, J. Org. Chem., 62 (1997) 1804–1809.

    Google Scholar 

  247. Zhang, H.-C., Brumfield, K.K. and Maryanoff, B.E., Synthesis of trisubstituted indoles on the solid-phase via palladium-mediated heterannulation of internal alkynes, Tetrahedron Lett., 38 (1997) 2439–2442.

    Google Scholar 

  248. Zuckermann, R.N., Kerr, J.M., Kent, S.B.H. and Moos, W.H., Efficient method for the preparation of peptoids [oligo(N-substituted glycines)] by submonomer solid-phase synthesis, J. Am. Chem. Soc., 114 (1992) 10646–10647.

    Google Scholar 

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Dolle, R.E. Comprehensive survey of combinatorial libraries with undisclosed biological activity: 1992–1997. Mol Divers 4, 233–256 (1998). https://doi.org/10.1023/A:1009653221320

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