Process to prepare n-[2-[(1s)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulphonyl) ethyl]-1, 3-dioxo-2,3-dihydro-1h-isoindol-4yl]acetamide

US10919855B2 · kind B2 · utility

Assignee

• Unichem Laboratories Ltd · IN

Inventors

• Dhananjay Govind Sathe · Mumbai, IN
• Arijit Das · Margao, IN
• Bhavesh B. Patel · Sayla, IN
• Dipak Subhash Patil · Jamkhed, IN
• Ashok Govind Matale · Jamkhed, IN
• Eknath Kamalakar Kshirsagar · Jamkhed, IN

Key dates

• Filing date: Apr 27, 2018
• Grant date: Feb 16, 2021
• Expiry date: Apr 27, 2038

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C317/28
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

An alternative and improved process for the preparation of Apremilast (Formula I) and Apremilast form B or a pharmaceutically acceptable salt thereof is provided. The novel process includes hydrogenation in acetone, Cyclization and acetylation followed by condensation in methyl isobutyl ketone (MIBK) and acetic acid mixture in specific volume ratios.