THE SYNTHESIS OF A CONFORMATIONALLY RESTRAINED, COMBINED THROMBOXANE ANTAGONIST/SYNTHASE INHIBITOR USING AN INTRAMOLECULAR STILLE-PALLADIUM-CATALYZED OR GRIGG-PALLADIUM-CATALYZED CYCLIZATION STRATEGY

被引:22
作者
FINCH, H
PEGG, NA
EVANS, B
机构
[1] Department of Medicinal Chemistry, Glaxo Group Research Ltd., Ware
关键词
D O I
10.1016/S0040-4039(00)61429-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of the conformationally restrained analogues 15 and 20, of the combined thromboxane antagonist / synthase inhibitor GR85305, has been achieved using novel intramolecular 'Stille'- and/or 'Grigg'-palladium-catalysed cyclisation reactions. A novel free radical cyclisation leading to an eight-membered ring is also described
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页码:8353 / 8356
页数:4
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