Synthesis process of ruxolitinib

US10562904B2 · kind B2 · utility

Assignee

• Chia Tai Tianqing Pharmaceutical Group Co., Ltd. · CN

Inventors

• Xiquan Zhang · 安丰镇, CN
• Aiming Zhang · Lianyungang, CN
• Zhou Zhou · Lianyungang, CN
• Leilei Yang · Lianyungang, CN
• Huadong Yao · Lianyungang, CN
• Xueyan Zhu · Shanghai, CN
• Hubo Wang · Shanghai, CN

Key dates

• Filing date: Dec 29, 2016
• Grant date: Feb 18, 2020
• Expiry date: Dec 29, 2036

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present application falls within the field of drug synthesis, and in particular, the present application relates to a method for preparing ruxolitinib, and a method for preparing the intermediate and relevant intermediates used. The method comprises reacting a compound of formula II with a compound of formula IV or a salt thereof to obtain a compound of formula III, and then subjecting the compound of formula III to an acyl halogenation reaction, an amidation reaction, and a reaction dehydrating an amide to form a cyano group or removing the protecting group to prepare ruxolitinib. The method has the characteristics of brief steps, a high stereoselectivity, a high utilization ratio of atoms, mild reaction conditions and convenient post treatment. The method avoids using expensive asymmetric reaction catalysts, and is suitable for industrial production.