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

被引:42
|
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
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
收藏
页码:4212 / 4215
页数:4
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