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三环稠合嘧啶并[4,5-b]吲哚-2-胺的简便合成方法。

A simple and facile synthesis of tricyclic-fused pyrimido[4,5-b]indol-2-amines.

机构信息

Institute of Superfine Chemicals, Bohai University, Keji Street, Jinzhou, 121000, People's Republic of China.

出版信息

Mol Divers. 2017 Nov;21(4):831-840. doi: 10.1007/s11030-017-9757-4. Epub 2017 Jun 19.

Abstract

In the present investigation, a simple and facile synthetic strategy for the construction of a series of structurally interesting tricyclic-fused N-alkyl-9H-pyrimido[4,5-b]indol-2-amines has been successfully achieved. Our synthesis, based on the annulation reaction between readily available 2-chloroindole-3-carbaldehydes or 3-acetyl-2-chloroindoles and guanidine nitrate using KOH as the base in refluxing EtOH medium, has the attractive features such as mild and economical reaction conditions and easy handing with lesser impact on the environment.

摘要

在本研究中,成功地实现了一种简单易行的合成策略,用于构建一系列结构有趣的三环融合 N-烷基-9H-嘧啶并[4,5-b]吲哚-2-胺。我们的合成方法基于在回流的 EtOH 介质中,使用 KOH 作为碱,将易得的 2-氯吲哚-3-甲醛或 3-乙酰基-2-氯吲哚与胍硝酸盐进行环合反应,具有温和、经济的反应条件,易于操作,对环境的影响较小等优点。

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