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Direct Acylation of Unactivated Alkyl Halides with Aldehydes through N-Heterocyclic Carbene Organocatalysis
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2023-08-15 , DOI: 10.1002/anie.202309572
Qing-Zhu Li 1 , Rong Zeng 1, 2 , Peng-Shuai Xu 1 , Xin-Hang Jin 1 , Chuan Xie 1 , Qi-Chun Yang 1 , Xiang Zhang 1 , Jun-Long Li 1
Affiliation  

Aldehydes underwent cross-coupling with unactivated alkyl halides in the presence of an NHC organocatalyst, thus enabling the rapid synthesis of various ketones from readily available starting materials under mild conditions. This method was also applied to the late-stage functionalization of pharmaceutical derivatives. Mechanistic investigations suggest a closed-shell nucleophilic substitution mechanism for this organocatalytic reaction.

中文翻译:

N-杂环卡宾有机催化未活化的卤代烷与醛的直接酰化

在 NHC 有机催化剂存在下,醛与未活化的卤代烷发生交叉偶联,从而能够在温和条件下从容易获得的起始材料快速合成各种酮。该方法也应用于药物衍生物的后期功能化。机理研究表明该有机催化反应存在闭壳亲核取代机制。
更新日期:2023-08-15
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