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
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机构:Department of Medicinal Chemistry, Glaxo Group Research Ltd., Ware
FINCH, H
PEGG, NA
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机构:Department of Medicinal Chemistry, Glaxo Group Research Ltd., Ware
PEGG, NA
EVANS, B
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机构:Department of Medicinal Chemistry, Glaxo Group Research Ltd., Ware
EVANS, B
机构:
[1] Department of Medicinal Chemistry, Glaxo Group Research Ltd., Ware
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