Solid-Phase Supported Synthesis: A Possibility for Rapid Scale-Up of Chemical Reactions

  • M. Meisenbach
  • T. Allmendinger
  • C.-P. Mak
Conference paper
Part of the Ernst Schering Foundation Symposium Proceedings book series (SCHERING FOUND, volume 2006/3)


The direct scale-up of a solid-phase synthesis has been demonstrated with 4-(2-amino-6-phenylpyrimidin-4-yl)benzamide and an arylsulfonamido-substituted hydroxamic acid derivative as examples. These compounds were obtained through combinatorial chemistry and solution-phase synthesis was used in parallel to provide a comparison. By applying highly loaded polystyrene-derived resins as the solid support, a good ratio between the product and the starting resin is achieved. We have demonstrated that the synthesis can be scaled up directly on the solid support, successfully providing the desired compounds easily and quickly in sufficient quantities for early development demands.


Hydroxamic Acid Reductive Amination Oxalyl Chloride Sodium Cyanoborohydride Imine Formation 
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Copyright information

© Springer-Verlag 2007

Authors and Affiliations

  1. 1.Chemical and Analytical DevelopmentNovartis Pharma AGBaselSwitzerland

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