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
收藏
页码：1549 / 1562
页数：14
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