Method for synthesizing kukoamine A and analogue thereof

The invention relates to the technical field of medicines, and relates to a method for synthesizing a natural product kukoamine A and analogue thereof. The method comprises the following steps: (1) performing a nucleophilic reaction on hydroxyl, halogen or C1-C10 alkoxy or C1-C10 alkyl substituted o...

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Hauptverfasser: Tian Ye, Zhang Hui, Liu Jianyu, Liu Yifeng, Xu Yongnan, Zhang Hefeng, Liu Dan, Zhan Yong, Zhao Qingchun, Chi Mingshuang, Ao Jiwei
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creator Tian Ye
Zhang Hui
Liu Jianyu
Liu Yifeng
Xu Yongnan
Zhang Hefeng
Liu Dan
Zhan Yong
Zhao Qingchun
Chi Mingshuang
Ao Jiwei
description The invention relates to the technical field of medicines, and relates to a method for synthesizing a natural product kukoamine A and analogue thereof. The method comprises the following steps: (1) performing a nucleophilic reaction on hydroxyl, halogen or C1-C10 alkoxy or C1-C10 alkyl substituted or unsubstituted benzaldehyde and malonic acid to obtain a compound 1; (2) reacting the compound 1 in the step (1) with N-hydroxy succinimide to obtain a compound 2; (3) reacting the compound 2 with spermine to obtain a compound 3; and (4) reacting the compound 3 with hydrogen to reduce carbon-carbon double bond, and purifying. The preparation method is simple, and provides a compound base to pharmacological activity research of compounds with similar structures. 本发明涉及医药技术领域,涉及天然产物地骨皮甲素及其类似物的合成方法。该方法包括:1)由羟基、卤素或C1-C10烷氧基或C1-C10烷基取代或未取代的苯甲醛与丙二酸进行亲核反应得化合物1;2)步骤1)所得化合物1和N-羟基琥珀酰亚胺反应,得化合物2;3)化合物2和精胺反应,得化合物3;4)化合物3用氢气反应以还原碳-碳双键,纯化即得。本发明制备方法简单,为类似结构化合物的药物活性研究提供了化合物基础。
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Method for synthesizing kukoamine A and analogue thereof
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