Transition-Metal-Free Decarboxylation of 3,3,3-Trifluoro-2,2-dimethylpropanoic Acid for the Preparation of C(CF3)Me2-Containing Heteroarenes,Organic Letters

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Transition-Metal-Free Decarboxylation of 3,3,3-Trifluoro-2,2-dimethylpropanoic Acid for the Preparation of C(CF3)Me2-Containing Heteroarenes
Organic Letters ( IF 4.9 ) Pub Date : 2018-08-27 00:00:00 , DOI: 10.1021/acs.orglett.8b02451
Shuai Liu ₁ , Yangen Huang ₁ , Feng-Ling Qing _{1,

2} , Xiu-Hua Xu ₂

Affiliation

The direct synthesis of C(CF₃)Me₂-substituted heteroarenes by decarboxylative 1,1-dimethyltrifluoroethylation of heteroarenes with 3,3,3-trifluoro-2,2-dimethylpropanoic acid is reported. This method does not need the transition-metal catalyst, and the base is crucial for this reaction. A series of previously unknown C(CF₃)Me₂-containing heteroarenes were obtained in high yields and have potential applications in the drug discovery process.

中文翻译：

3,3,3-三氟-2,2-二甲基丙酸的无过渡金属脱羧反应，用于制备含C（CF ₃）Me _2的杂芳烃

报道了通过杂芳烃与3,3,3-三氟-2,2-二甲基丙酸的脱羧1,1-二甲基三氟乙基化直接合成C（CF ₃）Me ₂取代的杂芳烃。该方法不需要过渡金属催化剂，碱对于该反应至关重要。以高收率获得了一系列先前未知的含C（CF ₃）Me ₂的杂芳烃，它们在药物发现过程中具有潜在的应用。

更新日期：2018-08-27

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