[EN] DECARBOXYLATIVE CONJUGATE ADDITIONS AND APPLICATIONS THEREOF<br/>[FR] ADDITIONS DE CONJUGUÉS AVEC DÉCARBOXYLATION ET APPLICATIONS ASSOCIÉES
申请人:UNIV PRINCETON
公开号:WO2016196931A1
公开(公告)日:2016-12-08
Synthetic methods are described herein operable to efficiently produce a wide variety of molecular species through conjugate additions via decarboxylative mechanisms. For example, methods of functionalization of peptide residues are described, including selective functionalization of peptide C-terminal residues. In one aspect, a method of peptide functionalization comprises providing a reaction mixture including a Michael acceptor and a peptide and coupling the Michael acceptor with the peptide via a mechanism including decarboxylation of a peptide reside.
本文描述了可操作的合成方法,能够通过脱羧机制通过共轭加成有效地产生各种分子物种。例如,描述了肽残基的官能化方法,包括对肽C-末端残基的选择性官能化。在一个方面,肽官能化方法包括提供包括迈克尔受体和肽的反应混合物,并通过包括肽残基的脱羧机制将迈克尔受体与肽偶联。