Author/Authors :
Liu، نويسنده , , Xiaoyu and Jiao، نويسنده , , Xiaozhen and Wu، نويسنده , , Qian and Tian، نويسنده , , Chengsen and Li، نويسنده , , Renze and Xie، نويسنده , , Ping، نويسنده ,
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.
Keywords :
Epoxide isomerization , Carbacyclic framework , Entecavir , Mitsunobu reaction
