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Short Paper | Regular issue | Vol 89, No. 12, 2014, pp.2806-2813
Published online, 5th December, 2014
DOI: 10.3987/COM-14-13117
A New and Practical Synthesis of Bosutinib

Han Wang, Chunping Zhu, Guoqing Zhu, Xin Tian, Yongjia Shen,* and Yongjun Mao*

*College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, 333 Longteng Rd., Songjiang, Shanghai, 201620, China

Abstract

New and improved synthetic route of bosutinib is described on a decagram scale. An intramolecular cyclization of 3-amino-2-(2-bromobenzoyl)- acrylonitrile (22) in K2CO3/DMF condition to form the key 3-cyano-4-hydroxyquinoline intermediate (13) is adopted as the key step. Bosutinib is obtained in 13.7% yield over ten steps and 98.9% purity (HPLC), which make it as a process of cost effective, environmentally friendly and feasible for scale-up operation.