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Short Paper | Regular issue | Vol 102, No. 9, 2021, pp.1803-1809
Published online, 2nd July, 2021
DOI: 10.3987/COM-21-14500
■ New Synthesis of Abexinostat

Xiaolei Zhu, Han Wang,* Sheng Lu, Cong Sun, Zhiyong Xu, and Jingli Xu

*College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201620, China

Abstract

A practical and convergent synthetic route of abexinostat was developed successfully. The key intermediate 3-((dimethylamino)methyl)- benzofuran-2-carboxylic acid (16) was prepared from 1-(2-hydroxyphenyl)ethan-1-one in 76.6% yield over 4 steps. Methyl 4-(2-aminoethoxy)benzoate hydrochloride (20) was synthesized from methyl 4-hydroxybenzoate in 97.0% yield over 2 steps. Abexinostat was obtained from 16 and 20 in 72.4% yield over 2 steps and 98.7% purity. Purification methods of the intermediates and the final product involved in the route were developed.