Facile access to polysubstituted Indoles via a cascade Cu-catalyzed arylation - Condensation process

被引:117
作者
Chen, Yu
Xie, Xiaoan
Ma, Dawei
机构
[1] Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Bioorganic & Nat Prod Chem, Shanghai 200323, Peoples R China
[2] Fudan Univ, Dept Chem, Shanghai 200433, Peoples R China
关键词
D O I
10.1021/jo702059q
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[Graphics] CuI/L-proline-catalyzed cross-coupling of 2-halotrifluoroacetanilides with beta-keto esters and amides followed by in situ acidic hydrolysis delivered 2,3-disubstituted indoles. The halides bearing a strong electron-withdrawing group in the 4-position can undergo in situ basic hydrolysis to provide the corresponding indoles. Polysubstituted indoles can be prepared from substituted 2-halotrifluoroacetanilides with high regioselectivity.
引用
收藏
页码:9329 / 9334
页数:6
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