Metal-free direct amidation of peptidyl thiol esters with α-amino acid esters†
Hao Chen,Maomao He,Yaya Wang,Linhui Zhai,Yongbo Cui,Yangyan Li,Yan Li,Haibing Zhou,Xuechuan Hong,Zixin Deng
Abstract
Metal-free direct amidation of peptidyl thiol esters with α-amino acid esters in the presence of bis(trimethylsilyl) acetamide (BSA) has been developed. This general method provides convenient access to N-protected peptides in good yields under mild conditions and demonstrates a high tolerance to functionality.