Nielsen Thomas E, Le Quement Sebastian T, Meldal Morten
Carlsberg Laboratory, SPOCC Centre, Gamle Carlsberg Vej 10, DK-2500 Valby, Denmark.
Org Lett. 2007 Jun 21;9(13):2469-72. doi: 10.1021/ol070693p. Epub 2007 May 23.
A general method for the solid-phase synthesis of carboxy-functionalized peptides by oxidative cleavage of alkynes is presented. Clean and quantitative conversion is enabled by the addition of bases, such as DABCO and HMTA, to the classical OsO4/NaIO4 mixture. The utility of the reaction is further illustrated by the synthesis of oxamic acids.
本文介绍了一种通过炔烃的氧化裂解进行羧基官能化肽固相合成的通用方法。向经典的OsO4/NaIO4混合物中添加碱(如DABCO和HMTA)可实现清洁且定量的转化。草氨酸的合成进一步说明了该反应的实用性。