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Total synthesis of Tasimelteon
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2019-06-25 , DOI: 10.1016/j.tetlet.2019.06.048
Xi-An Li , Lirong Yue , Jianrong Zhu , Huazhong Ren , Hong Zhang , Dong-yan Hu , Guangtian Han , Jiafu Feng , Ze-dong Nan

A simple and efficient approach has been accomplished for the total synthesis of active pharmaceutical ingredient (API) of Tasimelteon which is effective for treatment of non-24-h sleep-wake disorder. Starting from 4-vinyl-2, 3-dihydrobenzofuran, the synthesis involves asymmetric epoxidation, Wittig reaction, reduction of the nitrile group and propionation of the amine. The synthesis was accomplished in four steps in overall 48% yield.



中文翻译:

Tasimelteon的全合成

已经完成了一种简单有效的方法来完成Tasimelteon的活性药物成分(API)的总合成,该方法可有效治疗非24小时睡眠-觉醒障碍。从4-乙烯基-2,3-二氢苯并呋喃开始,合成涉及不对称环氧化,Wittig反应,腈基还原和胺的丙酸酯化。合成以四个步骤完成,总产率为48%。

更新日期:2019-06-25
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