A general synthesis of dioxolenone prodrug moieties
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- 作者：Sun ; Chong-Qing ; Cheng ; Peter T. W. ; Stevenson ; Jay ; Dejneka ; Tamara ; Brown ; Baerbel ; Wang ; Tammy C. ; et. al.
- 关键词：dioxolenone prodrug moieties ; phosphonate prodrugs ; squalene synthase inhibitors
- 刊名：Tetrahedron Letters
- 出版年：2002
- 出版时间：February 11, 2002
- 年：2002
- 卷：43
- 期：7
- 页码：1161-1164
- 全文大小：74.8 K
文摘
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.