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

Chemical and Pharmaceutical Bulletin, ISSN: 1347-5223, Vol: 64, Issue: 4, Page: 375-378
2016
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Article Description

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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