NEW AND CONVERGENT SYNTHESIS OF MOMELOTINIB DIHYDROCHLORIDE

作者：Zhao, Zhiwei; Liu, Mingjie; Liu, Yaowei; Wang, Yuan; Wu, Chuntao; Mao, Yongjun; Wang, Han^*; Xu, Jingli

来源：Heterocycles, 2018, 96(9): 1638-1643.

DOI：10.3987/COM-18-13961

• MYELOFIBROSIS

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).

• 出版日期2018-9-1
• 单位上海工程技术大学