Azepineindole alkaloid and preparation and anti-malarial application thereof

The invention provides anazepineindole alkaloid and a preparation method and an anti-malarial application thereof.The preparation method utilizes tryptamine and split ring strychnine as initial raw materials to obtain two diastereoisomers after being catalyzed and chemically modified by strictosidin...

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Hauptverfasser: ZOU HONGBIN, CAI YUNRUI, SHAO NANA
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides anazepineindole alkaloid and a preparation method and an anti-malarial application thereof.The preparation method utilizes tryptamine and split ring strychnine as initial raw materials to obtain two diastereoisomers after being catalyzed and chemically modified by strictosidinesynthetase and phosphoric acid.According to the method, two diastereoisomers of the azepineindole alkaloid are synthesized through a simple enzymatic chemical reaction and a purification method, a research shows that compounds and pharmaceutical salts thereof have outstanding anti-malarial activityand can be applied to the preparation of anti-malarial drugs.The structural formula of the two compounds is shown in the description. 本发明提供一种氮杂卓吲哚类生物碱及制备和抗疟疾用途,本发明利用色胺和裂环马钱子碱起始原料,通过异胡豆苷合成酶和磷酸催化、化学法修饰后得到二个非对映异构体。本发明通过简单酶化学反应和纯化方法,合成了两个氮杂卓吲哚类生物碱的非对映异构体,研究表明此类化合物及其可药用盐具有突出的抗疟疾活性,可在制备抗疟疾药物中进行应用。两个化合物具有以下结构式: