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Synthesis of Novel 5′-Hydrogenphosphonothioate Derivatives of AZT, d4T and ddI
Journal article   Peer reviewed

Synthesis of Novel 5′-Hydrogenphosphonothioate Derivatives of AZT, d4T and ddI

Ying Jin, Ming Sun, Hua Fu and Yu-Fen Zhao
Chemistry letters, Vol.33(2), pp.116-117
01/08/2004
Handle:
https://hdl.handle.net/20.500.12741/rep:10545

Abstract

5′-hydrogenphosphonothioate derivatives of AZT, d4T, and ddI as anti-HIV prodrug candidates were synthesized in 61–76% yields under mild conditions through sequential one-pot reactions, i.e., couple of triethylammonium phosphinate with different alcohols in the presence of pivaloyl chloride (PV-Cl), following oxidation with elemental sulfur and further condensation with AZT, d4T, or ddI in the presence of PV-Cl.

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