Method for preparing dabigatran etexilate intermediate, and intermediate compound

US10112901B2 · kind B2 · utility

Assignees

• SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY · CN
• China State Institute of Pharmaceutical Industry · CN
• Chia Tai Tianqing Pharmaceutical Group Co., Ltd. · CN

Inventors

• Yajun Guo · Shanghai, CN
• Hanbin Shan · County Road 325, CN
• Xueyan Zhu · Shanghai, CN
• Zhedong Yuan · Shanghai, CN
• Xiong Yu · Shanghai, CN
• Meng Guo · Shanghai, CN
• Mingtong Hu · Lianyungang, CN
• Duzheng Wang · Lianyungang, CN
• Yu Huang · Shanghai, CN

Key dates

• Filing date: Jul 3, 2014
• Grant date: Oct 30, 2018
• Expiry date: Jul 3, 2034

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D213/75
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Disclosed are a method for preparing a dabigatran etexilate intermediate, and an intermediate compound. The method for preparing a dabigatran etexilate intermediate 4 comprises: reacting a compound 3 with a C1-C3 alkyl alcohol solution of methylamine in an organic solvent, wherein, X=chlorine, bromine, or iodine. Also disclosed are an intermediate compound 3 and a preparation method thereof. The method for preparing a dabigatran etexilate intermediate of the present invention has the advantages of simple process, easy operation, high yield, and easy purification, thus being suitable for industrial production.