Process for making HIV protease inhibitors

US5663341A · kind A · utility

Assignee

• MERCK & CO., INC. · US

Inventors

• Kai Rossen · Hanau, DE
• David Askin · Hackettstown, US
• Paul J. Reider · Westfield, US
• Richard J. Varsolona · Scotch Plains, US
• Ralph P. Volante · Rahway, US

Key dates

• Filing date: Jun 7, 1995
• Grant date: Sep 2, 1997
• Expiry date: Jun 7, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A process for racemization of optically pure or enriched piperazine-2-tert-butylcarboxamide and its derivatives comprising reacting the optically pure or enriched piperazine compound with a racemizing agent selected from a strong base, an anhydrous metal salt or a carboxylic acid, in a solvent at a temperature range of between room temperature and 250.degree. C. The piperazine carboxamide derivatives are key intermediates in the preparation of HIV protease inhibitor compounds, including Compound J.