A novel and efficient synthesis of Entecavir |
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| Authors: | Xiaoyu LiuXiaozhen Jiao Qian WuChengsen Tian Renze LiPing Xie |
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| Affiliation: | State Key Laboratory of Bioactive Substance and Function of Natural Medicine, Beijing Key Laboratory of Active Substance Discovery and Drugability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Science & Pecking Union Medical College, No.1, Xiannongtan St., Beijing 100050, China |
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| Abstract: | A practical synthesis of Entecavir (1) has been accomplished in 10 steps with 21% overall yield. The key steps to construct the five-membered carbocyclic framework 2 are a ring-closing metathesis and a diethyl-aluminum 2,2,6,6-tetramethyl piperidide (DA-TMS) mediated epoxide isomerization. Furthermore, the guanine was introduced by modified Mitsunobu reaction. |
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| Keywords: | Entecavir Carbacyclic framework Epoxide isomerization Mitsunobu reaction |
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