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New Synthesis of Abexinostat
Heterocycles ( IF 0.8 ) Pub Date : 2021-07-02 , DOI: 10.3987/com-21-14500
Han Wang , Xiaolei Zhu , Sheng Lu , Cong Sun , Zhiyong Xu , Jingli Xu

A practical and convergent synthetic route of abexinostat was developed successfully. The key intermediate 3-((dimethylamino)methyl)- benzofuran-2-carboxylic acid (16) was prepared from 1-(2-hydroxyphenyl)ethan-1-one in 76.6% yield over 4 steps. Methyl 4-(2-aminoethoxy)benzoate hydrochloride (20) was synthesized from methyl 4-hydroxybenzoate in 97.0% yield over 2 steps. Abexinostat was obtained from 16 and 20 in 72.4% yield over 2 steps and 98.7% purity. Purification methods of the intermediates and the final product involved in the route were developed.

中文翻译:

Abexinostat 的新合成

成功开发了一条实用且趋同的abexinostat合成路线。关键中间体 3-((二甲氨基) 甲基)-苯并呋喃-2-羧酸 ( 16 ) 由 1-(2-羟基苯基)ethan-1-one 以 76.6% 的产率经过 4 个步骤制备。4-(2-氨基乙氧基)苯甲酸甲酯盐酸盐( 20 )从4-羟基苯甲酸甲酯以97.0%的产率经过2个步骤合成。Abexinostat 是从1620以 72.4% 的 2 步收率和 98.7% 纯度获得的。开发了该路线所涉及的中间体和最终产品的纯化方法。
更新日期:2021-07-02
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