Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Facile Preparation of Peptides with C-Terminal N-Alkylamide via Radical-Initiated Dethiocarboxylation
Tatsuhiko ShimizuRin MiyajimaNaoto NaruseKosuke YamaokaKeisuke AiharaAkira ShigenagaAkira Otaka
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2016 Volume 64 Issue 4 Pages 375-378

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Abstract

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.

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© 2016 The Pharmaceutical Society of Japan
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