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A general protocol for stereoselective construction of enaminyl sulfonyl fluorides
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2023-01-03 , DOI: 10.1039/d2qo01810a
Liu-Yang Chen 1 , K. P. Rakesh 2 , Hua-Li Qin 1
Affiliation  

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.

中文翻译:

烯胺基磺酰氟立体选择性构建的通用方案

开发了一种简单、高效且温和的 2-chloroprop-2-ene-1-sulfonyl fluoride (CESF) 与胺的反应,以良好至优异的产率 (56–96%) 提供多种高度官能化的烯胺基磺酰氟。这种转化具有广泛的底物范围、高原子经济性、操作简单和高达100%的立体选择性,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。
更新日期:2023-01-03
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