A new direction in peptide synthesis: an N-to-C approach using thioamides

酰胺键的合成是有机化学中最重要的技术之一。所有药品的65%的生产过程中形成了酰胺键，占该行业所有化学过程的六分之一。随着以酰胺键形成为中心支柱的多肽疗法的重要性日益增长，新的和有效的酰胺连接策略变得非常重要。该项目旨在开发基于羧酸和硫代酰胺的银促反应构建酰胺的新的合成方法。将开发氮到碳方向的多肽合成应用，有望实现碳末端修饰多肽的固相合成，如硫代酯。

The synthesis of amide bonds is one of the most important techniques in organic chemistry. Amide bonds are formed in the production of 65% of all pharmaceuticals, representing one sixth of all chemical processes in this industry. Coupled with the growing significance of peptide-based therapeutics, in which amide bond formation is the central pillar, novel and efficient amide ligation strategies are of great importance. This project aims to develop new synthetic methods for the construction of amides, based on the silver-promoted reaction of carboxylic acids and thioamides. Applications to the synthesis of peptides in the nitrogen-to-carbon direction will be developed, which are expected to enable solid-phase synthesis of carbon-terminally modified peptides, such as thioesters.