布朗斯特酸介导的由氧化锍叶立德合成噻唑。
Brønsted acid-mediated thiazole synthesis from sulfoxonium ylides.
作者信息
Smy Joe L, Ifill Roxanne, Hassell-Hart Storm
机构信息
Department of Chemistry, School of Life Sciences, University of Sussex, Brighton BN1 9QJ, UK.
出版信息
Chem Commun (Camb). 2024 Oct 22;60(85):12401-12404. doi: 10.1039/d4cc03905j.
PMID:39371008
Abstract
A Brønsted acid-mediated insertion of thioureas/thioamides into sulfoxonium ylides to synthesise 40 thiazoles (34-95% yields) under mild, metal-free conditions is described. This process is scalable, substrate-tolerant (including both α-substituted and heterocyclic ylides/groups) and was successfully applied to the late-stage functionalisation of the complex chemical probe molecule (+)-JQ1.
摘要
描述了一种布朗斯特酸介导的将硫脲/硫代酰胺插入到氧化锍叶立德中，在温和、无金属条件下合成40种噻唑（产率34 - 95%）的方法。该过程具有可扩展性、底物耐受性（包括α-取代的和杂环叶立德/基团），并成功应用于复杂化学探针分子(+)-JQ1的后期官能团化。
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