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

doi:10.1039/C1GC15401J

Metal-free direct amidation of peptidyl thiol esters with α-amino acid esters†

Hao Chen,^a Maomao He,^a Yaya Wang,^a Linhui Zhai,^a Yongbo Cui,^a Yangyan Li,^a Yan Li,^b Haibing Zhou,*^a Xuechuan Hong*^a and Zixin Deng^a

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^a Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education, and Wuhan University School of Pharmaceutical Sciences, Wuhan, P. R. China
E-mail: xhy78@whu.edu.cn, zhouhb@whu.edu.cn
Fax: +86 027-6875-9850
Tel: +86 027-6875-2331

^b State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, P. R. China

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.

Green Chemistry

Metal-free direct amidation of peptidyl thiol esters with α-amino acid esters†

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Metal-free direct amidation of peptidyl thiol esters with α-amino acid esters

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