Cp*Rh(III)-Catalyzed C-H 3,3-Difluoroallylation of Indoles and N-Iodosuccinimide-Mediated Cyclization for the Synthesis of Fluorinated 3,4-Dihydropyrimido-[1,6-a]indol-1(2H)-one Derivatives

被引：5

作者：

Zhao, Sen ^{[1
,2
,3
]}

Li, Chunpu ^{[2
,3
]}

Xu, Bin ^{[1
]}

Liu, Hong ^{[2
,3
]}

机构：

[1] Shanghai Univ, Coll Sci, Dept Chem, Shanghai 200444, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China

[3] Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 40卷 / 06期

基金：

中国国家自然科学基金;

关键词：

C-H activation; fluorine chemistry; rhodium catalysis; PROPARGYL ALCOHOLS; BOND ACTIVATION; ANNULATION; PHARMACEUTICALS; GENERATION; INHIBITORS; BENZAMIDES; PYRIDONES; POTENT;

D O I：

10.6023/cjoc202004039

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A mild and facile two-step strategy has been developed for the synthesis of fluorinated 3,4-dihydropyrimido-[1,6-a]-indol-1(2H)-ones through Cp*Rh(III)-catalyzed C-H 3,3-difluoroallylation and N-iodosuccinimide (NIS)-mediated cvclization. This strategy featured broad synthetic generality, unique versatility and high efficiency, which provided a potential tool for the construction of fluorine-containing heterocycles for drug discovery.

引用

页码：1549 / 1562

页数：14

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