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Preparation method of derivatives 3 - rented or C - alkylated from 2-hydroxy - 1,4 - naftoquinonas and analogues and preparation of lapachol

机译:由2-羟基-1,4-萘醌及其类似物的3-租或C-烷基化衍生物的制备方法和拉帕胆的制备。

摘要

Preparation method of derivatives 3 - rented or C - alkylated from 2-hydroxy - 1, 4 - naftoquinonas and analogues and preparation of lapachol.The present invention relates to a method for the preparation of alkylated derivatives 3 - or C - alkylated from 2-hydroxy - 1,4 - naftoquinonas and analogues and by means of this method the preparation of the natural product lapachol is the main intermediary to obtain the natural naphthoquinone 2 25 lapachona - (3,4 - diidro - 2, 2 - dimethyl 2H naphtho [1,2-b] Piran - 5.6 - Dione).This method of preparation of derivatives of 3 - rented or C - alkyl of 2 - hydroxy - 1,4 - naftoquinonas by reaction of reduction with formic acid to quinone metu00eddios generated by condensation with aldeidos (R ~ 5 ~ - CHO) in good chemical yields.In this patent application, we describe the results found for the preparation of various products obtained from type 1 or 2 - hydroxy - 1,4 - naftoquinonas replaced in position 3, including the natural product lapachol. The results indicated that the formic acid was effective in the reduction of quinones metu00eddios generated in the reaction medium.The structures of the products were confirmed by physical methods of analysis, with emphasis on the NMR of ^ 1 ^ H.
机译:由2-羟基-1,4-萘醌及其类似物3-租或C-烷基化的衍生物的制备方法和拉帕酚的制备。本发明涉及一种由2-羟基-烷基化的3-或C-烷基化的烷基化衍生物的制备方法。羟基-1,4-萘萘醌及其类似物,通过这种方法制备的天然产物拉帕酚是获得天然萘醌<2 25 lapachona>-(3,4--diidro-2,2-二甲基2H的主要中间体naphtho [1,2-b] Piran-5.6-Dione)。这种方法是通过用甲酸还原成醌的方法制备2-羟基-1,4-萘醌的3租或C-烷基衍生物的方法。与醛基(R〜5〜-CHO)缩合生成的u00eddios。在本专利申请中,我们描述了制备从1或2型羟基-1,4-萘醌取代的各种产品的结果。在位置3中,包括天然产品lapac霍尔。结果表明,甲酸能有效还原反应介质中生成的醌二甲醚。通过物理分析方法确定了产物的结构,重点是^ 1 ^ H的NMR。

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