Transition-Metal-Free Dehydrosilylative Difluoroamidation of Tetrahydroisoquinolines under Mild Conditions

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• 作者：Qiao Chen ; Jiawei Zhou ; Yanan Wang ; Chao Wang ; Xihong Liu ; Zhaoqing Xu ; Li Lin ; Rui Wang
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：September 4, 2015
• 年：2015
• 卷：17
• 期：17
• 页码：4212-4215
• 全文大小：400K
• ISSN：1523-7052

文摘

Disclosed herein is a dehydrosilylative difluoroamidation of 伪-Csp³鈥揌 of tetrahydroisoquinolines with 伪,伪-difluoro-伪-TMS-acetamides. The process, which occurs at ambient temperature in the absence of any transition metals, provides direct access to a broad range of 伪,伪-difluoroacetamide-substituted tertiary amine derivatives in high yields. Moreover, the method was successfully applied in the Csp³鈥揌-directed difluorophosphorylation and difluorocarboxylation under the same conditions.