1352145-46-0Relevant academic research and scientific papers
Entecavir intermediate and synthesis method thereof as well as method for synthesis of entecavir
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, (2019/05/15)
The invention relates to an entecavir intermediate and a preparation method thereof and a method for synthesis of entecavir by using the intermediate. The methods for synthesis of the entecavir and the entecavir intermediate have the advantages of controllable chirality, high yield and high product purity, raw materials are wide in source, reagents are cheap and easily available, the reaction is simple, the operation is simple and convenient, green and environment-friendly effects are achieved, and the method is suitable for industrial large-scale production.
Synthesis of Entecavir (BMS-200475)
Zhou, Bing,Li, Yuanchao
, p. 502 - 504 (2012/02/02)
A synthesis of Entecavir (BMS-200475) was achieved starting from 1,3-propanediol in 15 steps and 23.4% overall yield. A unique feature of the synthetic route is that the five-membered carbocyclic core is installed by an intramolecular nitrile oxide cycloaddition (INOC) reaction and the guanine moiety is introduced by a Mitsunobu reaction. The route is characteristic of low cost, high yield and easy operation.
