手性磷酸催化合成2-杂芳基取代的四氢喹啉
首发时间:2021-04-08
摘要:不对称催化一直是有机化学的热门研究方向。四氢喹啉是许多天然产物和生物活性分子的重要组成部分,开发新颖的有效方法用于构建高度对映体富集的四氢喹啉衍生物一直是学术界追求的目标。本文描述了在手性磷酸的催化下,实现了2-杂芳基取代的四氢喹啉的高效高选择性合成。以汉斯酯为氢源,邻二甲苯为溶剂,进行了底物范围拓展,以良好的产率和优异的对映选择性获得了一系列目标产物。该方法操作简便,具有环境友好性和原子经济性。
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Synthesis of 2-heteroaryl substituted tetrehydroquinlines catalyzed by chiral phosphoric acid
Abstract:Asymmetric catalysis has always been a hot research direction in organic chemistry. Tetrahydroquinoline is an important part of many natural products and biologically active molecules. The development of novel and effective methods for constructing highly enantiomerically enriched tetrahydroquinoline derivatives has always been the goal pursued by the academic community. This article describes the highly selective synthesis of 2-heteroaryl-substituted tetrahydroquinolines under the catalysis of chiral phosphoric acid. Using Hans ester as the hydrogen source and o-xylene as the solvent, the substrate range was expanded, and a series of target products were obtained with good yield and excellent enantioselectivity. The method is simple to operate, environmentally friendly and atomic economy.
Keywords: Asymmetric Catalysis Chiral phosphoric acid Hantzsch ester Tetrahydroquinoline
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