烯甲酰基磺酰基氟化物立体选择性构建的通用方案†

Liu-Yang Chen , K.P. Rakesh , Hua-Li Qin
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引用次数: 1

摘要

开发了一种简单、高效、温和的2-氯丙基-2-烯-1-磺酰基氟化物(CESF)与胺的反应,以良好至优异的产率(56–96%)提供了各种高度官能化的烯酰基磺酰基氟化物。该转化具有底物范围广、原子经济性高、操作简单、立体选择性高达100%的特点,在药物化学、化学生物学和药物发现方面具有巨大的应用价值。
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A general protocol for stereoselective construction of enaminyl sulfonyl fluorides†

A simple, efficient, and mild reaction of 2-chloroprop-2-ene-1-sulfonyl fluoride (CESF) with amines was developed, affording a variety of highly functionalized enaminyl sulfonyl fluorides in good to excellent yields (56–96%). This transformation features a broad substrate scope, high atom economy, operational simplicity and up to 100% stereoselectivity, which can provide great application value in medicinal chemistry, chemical biology, and drug discovery.

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CiteScore
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