新型3-氨基-2-苯甲酰基-1H-吲哚类衍生物的合成
Synthesis of a series new 3-amino-2-benzoyl-1H-indole derivatives
吲哚是一类具有广泛生物活性的含氮杂环化合物，作为药物分子设计与合成的基本砌块一直以来倍受药物化学研究者和有机合成工作者的青睐。本文报道了以邻氨基苯腈为起始原料，经酰胺化反应高收率得到N-(2-氰基苯基)氨基甲酸乙酯，再与α-溴代芳基乙酮进行Thorpe-Ziegler环化反应制得了3-氨基-1-乙酯基-2-苯甲酰基吲哚，最后经水解反应得到一系列新型标题化合物。该合成方法具有反应条件温和、易操作和产率高等优点，化合物的结构经MS和1HNMR的确认。
Indole which is the basic building block of drug design and organic synthesis, has been a very interesting and hot research area due to its broad-spectrum biological activities. In this paper, using 2-amino-benzonitrile as starting material, 3-amino-2-benzoyl-1H-indoles were prepared by amidation, Thorpe-Ziegler cyclization and hydrolysis reactions. The structures of target compounds were characterized by MS and 1H NMR. The method has some advantages of mild reaction conditions, easy operation and higher yield.
赵培亮、游文玮、胡孟金
药学制药化学工业生物化学
3-氨基吲哚合成horpe-Ziegler环化
3-amino-indolesynthesisThorpe-Ziegler Cyclization
赵培亮,游文玮,胡孟金.新型3-氨基-2-苯甲酰基-1H-吲哚类衍生物的合成[EB/OL].(2013-07-22)[2025-06-21].http://www.paper.edu.cn/releasepaper/content/201307-312.点此复制
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