Synthesis of 2-substituted-7-azaindoles from 2-amino-3-picolin

被引：11
|
作者：
Parcerisa, Javier [1 ]
Romero, Manel [1 ]
Dolors Pujol, Maria [1 ]
机构：
[1] Univ Barcelona, Fac Farm, Unitat Associada CSIC, Quim Farmaceut Lab, E-08028 Barcelona, Spain
来源：
TETRAHEDRON | 2008年 / 64卷 / 03期
关键词：
D O I：
10.1016/j.tet.2007.11.011
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
An easy route to the synthesis of 2-substituted-7-azaindole derivatives has been developed. The carbinol intermediate dissolved in DMF undergoes cyclization upon treatment with sodium hydride, trifluoroacetic anhydride, and trifluoroacetic acid at 120 degrees C in a straightforward and one-pot step. An alternative methodology using (CF3SO2)(2)O in acetonitrile in basic media followed by the addition of CF3COOH affords the expected 2-substituted azaindole in best yields. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：500 / 507
页数：8
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