一种由3-氨基-4-甲基吡啶和羧酸酯一步合成2-取代-6-氮杂吲哚的新方法。
A novel one-step synthesis of 2-substituted 6-azaindoles from 3-amino-4-picoline and carboxylic esters.
作者信息
Song Jinhua J, Tan Zhulin, Gallou Fabrice, Xu Jinghua, Yee Nathan K, Senanayake Chris H
机构信息
Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Old Ridgebury Road, P.O. Box 368, Ridgefield, Connecticut 06877-0368, USA.
出版信息
J Org Chem. 2005 Aug 5;70(16):6512-4. doi: 10.1021/jo0506480.
PMID:16050720
Abstract
Dilithiation of 3-amino-4-picoline (1) was achieved with sec-BuLi at room temperature. Condensation of the resulting dianion (2) with carboxylic esters afforded a wide range of 2-substituted 6-azaindoles in good yields.
摘要
在室温下，用仲丁基锂实现了3-氨基-4-甲基吡啶（1）的双锂化反应。所得双负离子（2）与羧酸酯缩合，以良好的产率得到了多种2-取代的6-氮杂吲哚。
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