137104-01-9Relevant academic research and scientific papers
Preparation of (±)-(erythro)-and (±)-(threo)-2-vinyl citric acids as potential mechanism-based inhibitors of ATP-citrate lyase
Dolle, Roland E.,Novelli, Riccardo,Saxty, Barbara A.,Wells, Timothy N. C.,Kruse, Lawrence I.,Camilleri, Patrick,Eggleston, Drake
, p. 4587 - 4590 (1991)
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.
