Copper-Mediated One-Pot Synthesis of 2,2-Difluoro-1,3-benzoxathioles from o-Bromophenols and Trifluoromethanethiolate,Organic Letters

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Copper-Mediated One-Pot Synthesis of 2,2-Difluoro-1,3-benzoxathioles from o-Bromophenols and Trifluoromethanethiolate
Organic Letters ( IF 4.9 ) Pub Date : 2018-01-08 00:00:00 , DOI: 10.1021/acs.orglett.7b03877
Mengjia Zhang ₁ , Shouxiong Chen ₁ , Zhiqiang Weng ₁

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A copper-mediated difluoromethylenation of o-bromophenols with trifluoromethanethiolate is described. This one-pot protocol proceeds through an intermolecular addition of S=CF₂ (resulting from the decomposition of trifluoromethanethiolate) to o-bromophenols followed by intramolecular C–S coupling to form 2,2-difluoro-1,3-benzoxathioles. This method is compatible with a broad range of substrates and enables the late-stage difluoromethylenation of several functionally dense druglike o-bromophenols.

中文翻译：

铜介导一锅从邻溴酚和三氟甲硫醇盐合成2,2-二氟-1,3-苯并草硫醇

描述了用三氟甲硫醇盐对邻溴苯酚进行铜介导的二氟亚甲基化。通过一分子间将S = CF ₂（由于三氟甲硫醇盐的分解而产生）加至邻溴酚中进行，然后分子内C-S偶联形成2，2-二氟-1,3-苯并草硫醇，这一一锅操作规程得以进行。该方法可与多种底物兼容，并且可以使几种功能密集的药物样邻溴苯酚进行后期二氟亚甲基化。

更新日期：2018-01-08

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