Method for preparing an important intermediate of linagliptin

US9522915B2 · kind B2 · utility

Assignee

• 2Y-CHEM, LTD. · CN

Inventors

• Yanfeng Zhou · Shanghai, CN
• Yong Liu · Shanghai, CN
• Xuezhang Wang · Shanghai, CN
• Xungui He · Shanghai, CN
• Yuan Wang · Hangzhou City, CN

Key dates

• Filing date: Oct 17, 2013
• Grant date: Dec 20, 2016
• Expiry date: Oct 17, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D473/06
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention discloses an improved process for preparing an important intermediate of linagliptin. In particular, disclosed are a process for preparing a compound V which is an important intermediate of linagliptin and has the structure V, and an industrial process of preparing linagliptin having excellent chemical and optical purities, which is an inhibitor of dipeptidyl peptidase-4 (DPP-IV), from the compound V. The process employs a phase-transfer catalyst, is high in yield, easy and simple to handle, environmentally friendly, suitable for industrial mass production, and can be implemented by a “one-pot process”.