Method for preparing 2-hydroxyl-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative

US10815208B2 · kind B2 · utility

Assignees

• INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES · CN
• TIANJIN CHASE SUN PHARMACEUTICAL CO. LTD · CN

Inventors

• Zhiqiang Feng · Changzhou City, CN
• Xiaoguang Chen · Beijing, CN
• Yang Yang · Parsippany, US
• Fangfang Lai · Beijing, CN

Key dates

• Filing date: May 23, 2017
• Grant date: Oct 27, 2020
• Expiry date: May 23, 2037

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C2601/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Provided is a method for preparing 2-hydroxy-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative represented by formula (I). The method comprises the following steps: (1) preparing 3-aryl-2-substituted toluene derivative 2 by using 3-iodo-2-substituted toluene derivative 1 and aryl boronic acid 5 or aryl boronate as starting materials; (2) preparing a benzyl halide derivative 3 by using 3-aryl-2-substituted toluene derivative 2 as starting materials; and (3) preparing 4-(2, 3-disubstituted benzyloxy)-2-hydroxy-5-substituted benzaldehyde derivative (I) by using benzyl halide derivative 3 and 2,4-dihydroxy-5-substituted benzaldehyde 6.