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Short Paper | Regular issue | Vol 96, No. 9, 2018, pp.1638-1643
Published online, 21st August, 2018
DOI: 10.3987/COM-18-13961
■ New and Convergent Synthesis of Momelotinib Dihydrochloride

Zhiwei Zhao, Mingjie Liu, Yaowei Liu, Yuan Wang, Chuntao Wu, Yongjun Mao, Han Wang,* and Jingli Xu

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

Abstract

A new and convergent synthesis of Momelotinib dihydrochloride, a new anticancer drug, is described in this article. The key step is cyclization of 1-(4-morpholinophenyl)guanidine (12) with N-(cyanomethyl)-4-(3-(dimethylamino)acryloyl)benzamide (17) to give Momelotinib under mild condition in 77% yield. The title product is obtained in 52.5% yield over 4 steps and 99.1% purity (HPLC).