期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 22, 期 11, 页码 1548-1552出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.8b00310
关键词
isosorbide-2-acetate; enzymatic synthesis; Novozym 435; lipase PS IM
资金
- Shandong New Time Pharmaceutical Co., Ltd.
- Biopharmaceutical Department of Shanghai State Institute of Pharmaceutical Industry
- Dr. Zhi-Jiang Jiang of Zhejiang University of Technology
Using immobilized lipase, we developed an enzymatic synthesis of isosorbide-2-acetate (1), a key intermediate in the preparation of isosorbide-5-mononitrate. 1 was prepared in high yield (similar to 92%) with excellent regioselectivity (>99.5% d.e.) through hydrolysis (Novozym 435) or alcoholysis (lipase PS IM) of isosorbide-2,5-diacetate. The conditions for the enzymatic process were optimized. The substrate concentration could be 400-500 g/L, and the enzyme to substrate ratio was <10 wt %. The feasibility of enzyme recycling was also demonstrated. In addition, the enzymatic process was carried out on a kilogram scale and was proved to be scalable, efficient, and economical.
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