Stereoselective Total Synthesis of Stereoisomers of Entecavir

Abstract

Practical methods for the synthesis of three stereoisomers of Entecavir have been developed. Starting from the reported intermediate (1S,2R)-2-((benzyloxy)methyl)cyclopent-3-en-1-ol and (1R,2S)-2-((benzyloxy)methyl)cyclopent-3-en-1-ol, respectively, three stereoisomers of Entecavir have been prepared with 17–20% overall yields. In principle, other stereoisomers could also be prepared by using the materials and reactions described in this article.

Key words

Entecavir - synthesis - stereoisomers - stereoselective - hepatitis B

Publication History

Received: 23 February 2023

Accepted after revision: 05 April 2023

Accepted Manuscript online:
05 April 2023

Article published online:
13 June 2023

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