Tetrahedron Letters

A novel and efficient synthesis of Entecavir

X Liu, X Jiao, Q Wu, C Tian, R Li, P Xie

文献索引：Liu, Xiaoyu; Jiao, Xiaozhen; Wu, Qian; Tian, Chengsen; Li, Renze; Xie, Ping Tetrahedron Letters, 2012 , vol. 53, # 29 p. 3805 - 3807

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被引用次数: 8

摘要

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.