Entecavir compound prepared in novel method

Abstract

The invention aims to provide an entecavir compound prepared in a novel method. The reaction procedures in the preparation method of the entecavir compound are simplified. Moreover, isopropyl is adopted as a protection agent. Since the steric hindrance can function as multiple types of directional substitution, the invention reduces the introduction of heterogeneous impurities. The reaction in multiple procedures needs no strict operating conditions. Therefore, the invention lays a foundation for industrial production.

Description

technical field [0001] The invention relates to a novel entecavir compound, which belongs to the technical field of medicine. Background technique [0002] Entecavir, chemical name 2-amino-9-[(1S,3S,4S)-4-hydroxy-3-hydroxymethyl-2-methylenepentyl]-1,9-hydrogen-6-H-purine- 6-keto-hydrate, molecular formula: C 12 h 15 N 5 o 3 ·H 2 O, molecular weight: 295.3, structural formula is [0003] [0004] Entecavir is a carbocyclic nucleoside anti-HBV drug developed by Bristol-Myers Squibb, which was approved by the US FDA in March 2005 for marketing in the US. Entecavir is a selective inhibitor of HBV DNA polymerase and blocks all three stages of HBV replication. Clinical studies have proved that entecavir has strong anti-HBV activity, which is significantly better than lamivudine and is still effective for patients who have failed lamivudine treatment. Entecavir is similar in safety and tolerability to lamivudine, but it is much less likely to develop clinical resistance ...

AI Technical Summary

Problems solved by technology

[0007] This route is relatively short, and the intermediate product page is relatively easy to purify, but the disadvantage is that it uses dimethylphenylchlorosilane as a protecting group and reacts at minus 78 ° C

Since dimethylphenylchlorosilane is not domestically produced, the import price is expensive, resulting in an increase in cost, and the resulting product has a low purity

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