Intermediates of sitagliptin and preparation process thereof

US9187419B2 · kind B2 · utility

Assignee

• ZHEJIANG HISOAR PHARMACEUTICAL CO., LTD. · CN

Inventors

• Xianhua Pan · Taizhou City, CN
• Weijin Li · Cameron Park, US
• Qunhui Zhang · Taizhou City, CN
• Libo Ruan · Taizhou City, CN
• Wansheng Yu · Taizhou City, CN
• Fei Deng · Folsom, US
• Tianhua Ma · Taizhou City, CN
• Mingwang Huang · Taizhou City, CN
• Minhuan He · Taizhou City, CN

Key dates

• Filing date: Dec 1, 2011
• Grant date: Nov 17, 2015
• Expiry date: Jan 18, 2032

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F7/10
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.