Pharmaceutical Chemistry Journal

, Volume 1, Issue 6, pp 303–306 | Cite as

Synthesis of pyrimidine analogs of folic acid

  • V. M. Berezovskii
  • G. D. Glebova
  • E. M. Birinberg
  • N. A. Andreeva


In order to study their antimetabolic activity, we have synthesized the 2-methyl-4-amino-, 2,4-diamino-, 2,6-diamino-4-hydroxy-, and 2,4-dihydroxypyrimidine analogs of folic acid from p-aminobenzoyl-L-glutamic acid and the corresponding substituted 5-bromomethyl-pyrimidines. The high antimetabolic activity of the 2,4-dihydroxypyrimidine analog in the inhibition of the reductases of folic and dihydrofolic acids and of the 2,4-diaminopyrimidine analog in the inhibition of the reductase of dihydrofolic acid has been shown.


Organic Chemistry Folic Acid Pyrimidine Pyrimidine Analog Dihydrofolic Acid 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

Literature cited

  1. 1.
    B. R. Baker and J. H. Jourdann, J. Heterocyclic Chem., No. 2, 162 (1965).Google Scholar
  2. 2.
    G. V. Chelintsev and D. E. Benevolenskaya, Zh. Obshch. Khim.,14, 1142 (1944).Google Scholar
  3. 3.
    G. Fodor, A. Gerech, I. Kishsh, et al., Zh. Obshch. Khim.,21, 1897 (1951).Google Scholar
  4. 4.
    Heterocyclic Compounds [in Russian], Vol. 6, Moscow (1960), p. 235.Google Scholar
  5. 5.
    L. J. Bellamy, Infrared Spectra of Complex Molecules, 2nd Ed., Methuen, London (1958).Google Scholar
  6. 6.
    N. A. Andreeva and R. I. Efimova, Dokl. Akad. Nauk SSSR,167, No. 4, 931 (1966).Google Scholar
  7. 7.
    N. A. Andreeva, A. V. Sergeev, and R. I. Efimova, Dokl. Akad. Nauk SSSR,168, No. 1, 204 (1966).Google Scholar
  8. 8.
    G. M. Timmis and D. G. J. Felton, J. Pharm. (London),9, 46 (1957).Google Scholar
  9. 9.
    J. A. Montgomery, Cancer Res.,19, 447 (1959).Google Scholar
  10. 10.
    B. Pulman and A. Pulman, Quantum Biochemistry [Russian translation], Moscow (1965).Google Scholar
  11. 11.
    J. A. Carbon, J. Org. Chem.,25, 1731 (1960).Google Scholar

Copyright information

© Consultants Bureau 1968

Authors and Affiliations

  • V. M. Berezovskii
    • 1
  • G. D. Glebova
    • 1
  • E. M. Birinberg
    • 1
  • N. A. Andreeva
    • 1
  1. 1.All-Union Scientific Research Vitamin InstituteMoscow

Personalised recommendations