Process for the preparation of vincamine
    3.
    发明授权
    Process for the preparation of vincamine 失效
    长春胺的制备方法

    公开(公告)号:US3884927A

    公开(公告)日:1975-05-20

    申请号:US34525573

    申请日:1973-03-27

    Applicant: ROUSSEL UCLAF

    CPC classification number: C07D461/00

    Abstract: Process for the preparation of vincamine wherein eburnamonine is reacted with an ethynylmagnesium halide to give (20 Alpha ,21 Alpha ) 16 Alpha -ethynyl eburnane 16 Beta -ol, which upon oxidation to vincaminic acid and subsequent methylation provides vincamine. The optically active forms of vincamine can be obtained by using an optically active form of eburnamonine.

    Abstract translation: 用于制备长春胺的方法,其中将本香糖胺与乙炔基卤化镁反应,得到[20α,21α]16α-乙炔基伊本烷16β-醇,其在氧化为半胱氨酸并随后甲基化时提供长春胺。 长春胺的光学活性形式可以通过使用光学活性形式的eburnamonine来获得。

    Derivatives of 9h-pyrido(3,4-b) indole and process of preparation
    4.
    发明授权
    Derivatives of 9h-pyrido(3,4-b) indole and process of preparation 失效
    9H-吡啶(3,4-B)吲哚的衍生物及其制备方法

    公开(公告)号:US3862160A

    公开(公告)日:1975-01-21

    申请号:US38206173

    申请日:1973-07-24

    Applicant: ROUSSEL UCLAF

    Abstract: The preparation of derivatives of 1,2,3,4-tetrahydro-9H-pyrido (3,4-b) indole is described. In particular the preparation of acrylic esters of Beta -(3''-hydroxypropyl)-1,2,3,4-tetrahydro9H-pyrido (3,4-b) indole is shown to proceed from the oxidation of a 2-alkyloxy-3-hydroxytetrahydropyran to its 2-alkyloxy-3oxotetrahydropyran derivative. The Wittig condensation is used to effect the reaction of this ketone with a phosphonoacetic ester giving rise to the carbalkoxy methylenic-substitution product, 2alkyloxy-3-(1''-alkoxycarbonyl)methylidenetetrahydropyran. After acid hydrolysis of the 2-alkyloxy group, condensation is carried out with tryptamine resulting in the desired indole derivatives. Such compounds can be used in the facile preparation of alkaloids of the eburnamonie family.

    Abstract translation: 描述了1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚衍生物的制备。 具体地说,β-(3'-羟丙基)-1,2,3,4-四氢-9H-吡啶并[3,4-b]吲哚的丙烯酸酯的制备显示出从2-烷氧基 -3-羟基四氢吡喃与其2-烷氧基-3-氧代四氢吡喃衍生物。 维t嗪缩合用于使该酮与一种膦酰基乙酸酯反应,生成2-烷氧基-3-(1'-烷氧基羰基)亚甲基四氢吡喃的烷氧基亚甲基取代产物。 在2-烷氧基酸水解后,用色胺进行缩合,产生所需的吲哚衍生物。 这些化合物可用于易燃鳗ie族家族生物碱的制备。

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