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Design and synthesis of novel fluoro amino acids: synthons for potent macrocyclic HCV NS3 protease inhibitors

✍ Scribed by Latha G. Nair; Stephane Bogen; Frank Bennett; Kevin Chen; Bancha Vibulbhan; Yuhua Huang; Weing Yang; Ronald J. Doll; N.-Y. Shih; F. George Njoroge

Book ID: 104097702
Publisher: Elsevier Science
Year: 2010
Tongue: French
Weight: 952 KB
Volume: 51
Category: Article
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2010.04.010

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✦ Synopsis

The Hepatitis C Virus (HCV) is a major health hazard and its infection is a leading cause of chronic liver disease world wide. In our efforts toward the discovery of a back up to our first clinical candidate, Boceprevir (SCH 503034), we approached the depeptidization of the molecule through macrocyclization. Herein we report the design and synthesis of fluoro amino acids with desired stereochemistry required for the synthesis of macrocyclic inhibitors with fluorine at various positions of the aliphatic chain. Biological activities of representative examples are also reported.

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