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The synthesis of 3??hydroxymethyldibenzo [b, f] thiepin 5, 5??dioxide, a prostaglandin antagonist

D Hands, H Marley, SJ Skittrall…

文献索引:Hands; Marley; Skittrall; Wright Journal of Heterocyclic Chemistry, 1986 , vol. 23, # 5 p. 1333 - 1337

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被引用次数: 2

摘要

Abstract An economic synthesis of 3-hydroxymethyldibenzo [b, f] thiepin 5, 5-dioxide, a novel prostaglandin antagonist, is described. The key step in the synthesis is the formation of a carboxyphenylacetic acid by carboxylation of a toluic acid dianion, followed by cyclisation to the tricyclic ketone. Readily available starting materials are used in the synthesis and conditions have been found at each stage to give pure intermediates, requiring little ...