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Base-Catalyzed Selective Deuteration of Alkynes
Asian Journal of Organic Chemistry ( IF 2.7 ) Pub Date : 2021-08-10 , DOI: 10.1002/ajoc.202100405
Akhilesh Kumar Verma 1 , Shiv Kumar 2 , Monika Patel 3
Affiliation  

Deuteration of organic molecules has gained considerable importance in medicinal chemistry. A mild concept of inducing 2H isotope stoichiometrically into terminal alkynes has been developed using KOH-DMSO-d6 medium. The four pairs of substrate scopes, namely aromatic, aliphatic, dialkynes, and alcohol/amine-substituted alkyne were readily switchable from hydrogen to deuterium. Mild reaction condition, no requirement of column chromatography; environment-friendly nature of the protocol increases the synthetic utility of the developed chemistry. The developed procedure avoids the use of expensive transition-metal catalysts and should find attention in academia as well as in pharmaceuticals.
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中文翻译:

炔烃的碱催化选择性氘化

有机分子的氘化在药物化学中具有相当重要的意义。已经使用 KOH-DMSO- d 6介质开发了将2 H 同位素化学计量地引入末端炔烃的温和概念。四对底物范围,即芳香族、脂肪族、二炔和醇/胺取代的炔很容易从氢转换为氘。反应条件温和,无需柱层析;该议定书的环保性质增加了已开发化学的合成效用。所开发的程序避免使用昂贵的过渡金属催化剂,应引起学术界和制药业的关注。
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更新日期:2021-09-13
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