Deuterated hepatitis C protease inhibitors

US8247532B2 · kind B2 · utility

Assignee

• Vertex Pharmaceuticals Incorporated · US

Inventors

• Robert B. Perni · Marlborough, US
• Youssef L. Bennani · Village of La Jolla, US
• Gregor Zlokarnik · Village of La Jolla, US
• Gerald J. Tanoury · Marlborough, US
• Minzhang Chen · Acton, US
• Young Chun Jung · Lexington, US
• Raymond E. Forslund · Natick, US
• Francois Maltais · Somerville, US

Key dates

• Filing date: Nov 24, 2010
• Grant date: Aug 21, 2012
• Expiry date: Nov 24, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

This invention relates to processes and intermediates for the preparation of salts of deuterated, enantiomericallv enriched alpha-amino beta-hydroxy acids of Formula 1wherein the variables R1,R′1 and R′2 are defined herein, and wherein the process may comprise the steps of forming a salt of a compound of Formula 1, and crystallizing said salt to give a compound of greater than 55% enantiomeric excess.