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

被引：45

作者：

Chen, Qiao ^{[1
]}

Zhou, Jiawei ^{[1
]}

Wang, Yanan ^{[1
]}

Wang, Chao ^{[1
]}

Liu, Xihong ^{[1
]}

Xu, Zhaoqing ^{[1
]}

Lin, Li ^{[1
]}

Wang, Rui ^{[1
]}

机构：

[1] Lanzhou Univ, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, Lanzhou 730000, Peoples R China

来源：

ORGANIC LETTERS | 2015年 / 17卷 / 17期

关键词：

H BOND FUNCTIONALIZATION; CARBON-HYDROGEN BONDS; TERTIARY-AMINES; NITROGEN ATOM; MEDICINAL CHEMISTRY; CATALYZED ARYLATION; VERSATILE APPROACH; BETA-KETOESTERS; TRIFLUOROMETHYLATION; DIFLUOROMETHYLATION;

D O I：

10.1021/acs.orglett.5b01997

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Disclosed herein is a dehydrosilylative difluoroamidation of alpha-Csp(3)-H of tetrahydroisoquinolines with alpha,alpha-difluoro-alpha-TMS-acetamides. The process, which occurs at ambient temperature in the absence of any transition metals, provides direct access to a broad range of alpha,alpha-difluoroacetamide-substituted tertiary amine derivatives in high yields. Moreover, the method was successfully applied in the Csp(3)-H-directed difluorophosphorylation and difluorocarboxylation under the same conditions.

引用

页码：4212 / 4215

页数：4

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