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    • 60. 发明授权
    • Process for the preparation of eburnamonine derivatives
    • 制备苯丙胺衍生物的方法
    • US4464535A
    • 1984-08-07
    • US438288
    • 1982-11-01
    • Csaba SzantayLajos SzaboGyorgy KalausJanos KreidlGyorgy ViskyAndras NemesLaszlo CzibulaMaria Farkas nee Kirjak
    • Csaba SzantayLajos SzaboGyorgy KalausJanos KreidlGyorgy ViskyAndras NemesLaszlo CzibulaMaria Farkas nee Kirjak
    • C07D461/00C07D471/14C07D455/00
    • C07D471/14C07D461/00
    • The invention relates to a new process for the preparation of eburnamonine derivatives of the general Formula I ##STR1## (wherein R.sup.1 is an alkyl group having 1-6 carbon atoms) and optical and geometrical isomers thereof which comprises reacting a hydroxyimino-octahydro-indolo[2,3-a]quinolizine derivative of the general Formula II ##STR2## (wherein R.sup.1 is as stated above and R.sup.2 stands for an alkyl group having 1-6 carbon atoms being identical with or different from R.sup.1, or a hydrogen atom) or an acid addition salt thereof in an organic protic solvent or solvent mixture with an inorganic base, optionally under the addition of water or an aqueous mineral acid, at a temperature between 60.degree. C. and 200.degree. C.The compounds of the present invention are known drugs having blood pressure decreasing and cerebral vasodilatatory effect. The advantage of the process of the present invention is that it is readily feasible on industrial scale too, provides isomer-free pure products with high yield and requires the use of readily available simple starting materials.
    • 本发明涉及一种制备通式Ⅰ(I)(Ⅰ)(其中R1是具有1-6个碳原子的烷基)及其光学和几何异构体的本发明化合物的新方法,其包括使羟基亚氨基 - 通式II的八氢 - 吲哚并[2,3-a]喹嗪衍生物(II)(其中R 1如上所述,R 2表示具有1-6个碳原子的烷基,与R 1相同或不同) ,或氢原子)或其酸加成盐在无机碱的有机质子溶剂或溶剂混合物中,任选在水或无机酸水溶液中,在60℃至200℃的温度下进行。 本发明的化合物是具有降血压和脑血管扩张作用的已知药物。 本发明方法的优点是在工业规模上也容易实现,提供高产率的无异构体纯产品,并且需要使用容易获得的简单起始原料。