SYNTHESIS VIA VINYL SULFONES .32. TRIPLY-CONVERGENT SYNTHESES OF 2 HOMOCHIRAL ARENE-FUSED PROSTACYCLIN ANALOGS RELATED TO U68,215

被引：10

作者：

HARDINGER, SA ^{[1
]}

JAKUBOWSKI, JA ^{[1
]}

FUCHS, PL ^{[1
]}

机构：

[1] ELI LILLY & CO,DEPT CARDIOVASC PHARMACOL,INDIANAPOLIS,IN 46285

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)81097-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The syntheses of arene-fused prostacyclin analogs 2 and 3 are described. Rapid assembly of the tricyclic skeleton is achieved in a triply-convergent manner from oxazoline-bearing homocuprate 6b, homochiral ammonium salt Z and homochiral propargyl acetylide 12. Compound 2 was a potent inhibitor of collagen-induced platelet aggregation having an IC50 = 2.9nM; while 3 exhibited an IC50 = 52nM.

引用

页码：79 / 82

页数：4

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