首页> 外国专利> DERIVATIVE OF 14-HYDROXYNJRMORPHINONE, DERIVATIVE OF MORPHINONE, DERIVATIVE OF MORPHINE, METHODS FOR PREPARING DERIVATIVE OF 14-HYDROXYNORMORPHINONE, DERIVATIVE OF MORPHINONE, NOROXYMORPHONE

DERIVATIVE OF 14-HYDROXYNJRMORPHINONE, DERIVATIVE OF MORPHINONE, DERIVATIVE OF MORPHINE, METHODS FOR PREPARING DERIVATIVE OF 14-HYDROXYNORMORPHINONE, DERIVATIVE OF MORPHINONE, NOROXYMORPHONE

机译:14-羟基吗啡酮的衍生物,吗啡酮的衍生物,吗啡的衍生物,14-羟基吗啡酮的衍生物的制备方法,吗啡酮,去甲羟吗啡酮

摘要

FIELD: organic chemistry, chemical technology.;SUBSTANCE: invention relates to compounds, namely, to derivative of 14-hydrxoynormorphinone of the formula (IV) , derivative of morphinone of the formula (III) , derivative of morphine of the formula (II) wherein R1 represents (C1-C7)-alkyl; R2 represents benzyl or benzyl substituted with one or some (C1-C6)-alkoxy-groups, or benzyl substituted with one or some halogen atom. Also, invention relates to a method for synthesis of derivative of 14-hydroxynormorphinone of the formula (IV) involving interaction of compound of the formula (III) with cobalt (II) as oxidant in the presence of a weak base and air or oxygen as co-oxidant. Also, invention relates to a method for synthesis of derivative of morphinone of the formula (III) involving interaction of derivative of morphine of the formula (II) with oxidizing agent that is effective in oxidation of allyl hydroxy-groups. Mainly, invention relates to a method for synthesis of noroxymorphone. The process involves oxidation of derivative of morphinone of the formula (III) to derivative of 14-hydroxynormorphinone of the formula (IV), removal of protection from 3-position and reduction of double bond at 7,8-position in derivative of 14-hydroxynormorphinone of the formula (IV) to yield derivative of 3,14-hydroxynormorphinone of the formula (V) and hydrolysis of derivative of 3,14-hydroxynormorphinone of the formula (V) to yield noroxymorphone of the formula (VI) wherein formulae (V) and (VI) are given in the invention description. Invention provides synthesis of noroxymorphone using novel intermediate compounds.;EFFECT: improved method of synthesis.;25 cl, 1 sch, 1 ex
机译:技术领域:有机化学,化学技术。发明领域:本发明涉及化合物,即涉及式(IV)的14-羟基去甲吗啡酮的衍生物。,式(III)吗啡酮的衍生物<图像文件=“ 00000005.GIF” he =“ 26” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 47” />,式(II)的吗啡衍生物<图像文件=“ 00000006.GIF” he =“ 26” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 46” />其中R 1 < / Sub>表示(C 1 -C 7 )-烷基; R 2 表示苄基或被一个或某些(C 1 -C 6 )-烷氧基取代的苄基,或被一个或多个取代的苄基一些卤素原子。另外,本发明涉及一种合成式(IV)的14-羟基降吗啡酮的衍生物的方法,该方法包括在弱碱和空气或氧气存在下,式(III)的化合物与作为氧化剂的钴(II)的相互作用。助氧化剂。另外,本发明涉及一种合成式(III)的吗啡酮的衍生物的方法,该方法涉及式(II)的吗啡的衍生物与对烯丙基羟基的氧化有效的氧化剂的相互作用。本发明主要涉及去甲羟吗啡酮的合成方法。该方法包括将式(III)的吗啡酮的衍生物氧化为式(IV)的14-羟基降吗啡酮的衍生物,除去3-位的保护作用,并还原14-的衍生物中7,8-位的双键。式(IV)的羟基去甲吗啡酮产生式(V)的3,14-羟基去甲吗啡酮的衍生物和式(V)的3,14-羟基去甲吗啡酮的衍生物的水解以产生式(VI)的去甲吗啡酮V)和(VI)在发明说明书中给出。本发明提供了使用新型中间体化合物合成去甲羟吗啡酮的作用;效果:改进的合成方法; 25 cl,1 sch,1 ex

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