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Synthesis 2023; 55(19): 3109-3112
DOI: 10.1055/a-2069-4552
DOI: 10.1055/a-2069-4552
paper
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.
Supporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/a-2069-4552. Included are 2D HSQC, 2D HMBC, 2D H,H-COSY, and 2D H,H-NOE analyses.
- Supporting Information
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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