PREPARATION OF (+/-)-(ERYTHRO)-2-VINYLCITRIC AND (+/-)-(THREO)-2-VINYLCITRIC ACIDS AS POTENTIAL MECHANISM-BASED INHIBITORS OF ATP-CITRATE LYASE

被引：7

作者：

DOLLE, RE ^{[1
]}

NOVELLI, R ^{[1
]}

SAXTY, BA ^{[1
]}

WELLS, TNC ^{[1
]}

KRUSE, LI ^{[1
]}

CAMILLERI, P ^{[1
]}

EGGLESTON, D ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,THE FRYTHE,WELWYN GARDEN CIT AL6 9AR,HERTS,ENGLAND

来源：

TETRAHEDRON LETTERS | 1991年 / 32卷 / 35期

关键词：

D O I：

10.1016/0040-4039(91)80046-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The dianion of diethyl-1,3-acetone dicarboxylate 6 was reacted with a vinyl cation equivalent, 2-bromoethyl phenyl selenide, to give the mono alkylated 3-oxoglutarate 7 in 80% yield. Subsequent four-step elaboration gave the title citric acid analogues. These agents were designed as potential mechanism-based inhibitors of ATP-citrate lyase, an enzyme involved in cholesterol and lipid biosynthesis.

引用

页码：4587 / 4590

页数：4

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