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Original Articles

A Phosphoramidite-Based Synthesis of Phosphoramidate Amino Acid Diesters of Antiviral Nucleosides

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Pages 1891-1903 | Received 14 Jan 1994, Accepted 02 May 1994, Published online: 24 Sep 2006
 

Abstract

A general synthetic procedure is presented for the preparation of 5′-amino acid phosphoramidates of zidovudine (AZT), 3′-deoxy-2′,3′-didehydrothymidine (D4T), and 3′-fluoro-3′-deoxythymidine (FLT) from their corresponding phosphoramidites. These water soluble amino acid phosphoramidates are more non-polar than the parent nucleoside and exhibit high stability in aqueous media.

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