Laboratory for Bioorganic Chemistry, Sloan-Kettering Institute for Cancer Research, 1275 York Avenue, New York, NY 10065, USA.
Angew Chem Int Ed Engl. 2010 Dec 3;49(49):9500-3. doi: 10.1002/anie.201005513.
[Image: see text] An efficient and broadly useful two-step ligation protocol is developed. Important mechanistic issues of ligation were probed from diastereomeric competition studies on the formation of the ligation products. We also report an instance of kinetically controlled ligation through the exploitation of selectivity differences between related N-termini. This study potentially provides a valuable approach to facilitate polypeptide synthesis by minimizing protecting group manipulations and intermediate isolations..
[图片：见正文] 开发了一种高效且广泛适用的两步连接方案。通过对连接产物形成的非对映体竞争研究，探讨了连接中的重要机制问题。我们还报告了通过利用相关 N 端之间的选择性差异来实现动力学控制连接的实例。该研究通过最小化保护基操作和中间分离，为促进多肽合成提供了一种有价值的方法。
