Sitagliptin synthesis

US8846916B2 · kind B2 · utility

Assignee

• Generics [UK] Limited · GB

Inventors

• Vinayak Govind Gore · Panvel, IN
• Maheshkumar Gadakar · Jamkhed, IN
• Priyanka Bhosle · Jamkhed, IN
• Suresh Shinde · Jamkhed, IN

Key dates

• Filing date: May 10, 2010
• Grant date: Sep 30, 2014
• Expiry date: May 10, 2030

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07B2200/07
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.