A general method for acylation of indoles at the 3-position with acyl chlorides in the presence of dialkylaluminum chloride

被引:151
作者
Okauchi, T
Itonaga, M
Minami, T
Owa, T
Kitoh, K
Yoshino, H
机构
[1] Kyushu Inst Technol, Dept Appl Chem, Kitakyushu, Fukuoka 8048550, Japan
[2] Eisai & Co Ltd, Tsukuba Res Labs, Tsukuba, Ibaraki 3002635, Japan
关键词
D O I
10.1021/ol005841p
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] Indoles are selectively acylated at the a position in high yields on treatment with a wide variety of acyl chlorides in CH2Cl2 in the presence of diethylaluminum chloride or dimethylaluminum chloride. The reaction proceeds under mild conditions and is applicable to indoles bearing various functional groups without NH protection.
引用
收藏
页码:1485 / 1487
页数:3
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