摘要

In seeking to develop an iterative approach to the preparation of alpha-oligopeptides by the chemoselective amide-forming coupling of alpha-ketoacids and hydroxylamines, we have designed and synthesized novel enantiopure monomers. Key to our approach is the use of alpha,alpha-dichloroacids as masked alpha-ketoacids. The preparation of these monomers, their coupling with alpha-ketoacids, and the conversion of the alpha,alpha-dichloroacids to alpha-ketoacids is described. These studies provide a first step to a conceptually unique approach to peptide synthesis that does not require activating reagents or produce chemical byproducts.

  • 出版日期2011-3-1