A general synthesis of dioxolenone prodrug moieties

…, PTW Cheng, J Stevenson, T Dejneka, B Brown…

Index: Sun, Chong-Qing; Cheng, Peter T.W.; Stevenson, Jay; Dejneka, Tamara; Brown, Baerbel; Wang, Tammy C.; Robl, Jeffrey A.; Poss, Michael A. Tetrahedron Letters, 2002 , vol. 43, # 7 p. 1161 - 1164

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Citation Number: 22

Abstract

A general method for the synthesis of dioxolenone prodrug moieties from appropriately substituted β-ketoesters is described. This novel and versatile sequence allows for the synthesis of alkyl-or aryl-substituted dioxolenone alcohols 8 or bromides 9. Coupling of the bromides 9 to prepare bis-dioxolenone phosphonate prodrug esters is also presented.