Facile Preparation of Peptides with C-Terminal N-Alkylamide via Radical-Initiated Dethiocarboxylation.

A new synthetic method has been developed to prepare peptides bearing a C-terminal N-alkylamide from peptide thioacids via a radical-initiated dethiocarboxylation process. This method enables the introduction of various alkyl groups to C-terminal amides simply by replacing the amino acid building block. Its application to the preparation of anti-cancer drug ABT-510 is also reported.

Citation

Tatsuhiko Shimizu, Rin Miyajima, Naoto Naruse, Kosuke Yamaoka, Keisuke Aihara, Akira Shigenaga, Akira Otaka. Facile Preparation of Peptides with C-Terminal N-Alkylamide via Radical-Initiated Dethiocarboxylation. Chemical & pharmaceutical bulletin. 2016;64(4):375-8

PMID: 27039836

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