New synthesis route for the preparation of pomalidomide

Daowei HuangNovel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, China;Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, China

Chengwu ShenShandong Provincial Hospital, Shandong University, Jinan, China

Wenya WangNovel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, China;Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, China

Lei HuangNovel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, China;Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, China

Feng NiNovel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, China;Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, China

Jianqi LiNovel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai, China;Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai, ChinaCorrespondence[email protected]

ABSTRACT

A new route for the preparation of pomalidomide is described in the study. The synthetic procedure starts from 4-nitroisobenzofuran-1,3-dione and 3-aminopiperidine-2,6-dione hydrochloride via a three-step reaction resulting in a total yield of 65% with a high-performance liquid chromatographic (HPLC) purity of 99.56% and a low palladium residue level of 2 ppm. This method can be deemed as an efficient, practical, and environmentally friendly synthetic route for the preparation of pomalidomide.

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New synthesis route for the preparation of pomalidomide

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New synthesis route for the preparation of pomalidomide

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