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A method for the production of zolmitriptanverbindungen

机译:一种生产佐米曲坦丹佛龙的方法

摘要

In particular, zolmitriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Transesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Saponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Decarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.
机译:尤其是佐米曲普坦或其药学上可接受的盐,其包括:a)制备苯胺盐酸盐(II)的重氮盐;然后还原和酸化得到肼(III); b)使盐酸肼(Ⅲ)与α-酮-β-戊内酯原位反应,得到the(Ⅳ)。 c)费歇尔吲哚合成the(IV),得到式(V)的吡喃吲哚酮; d)吡喃吲哚酮(V)的酯交换反应得到化合物(VI),其中R是指直链或支链的C1-C4烷基; e)将化合物(Ⅵ)的羟基转化成二甲氨基,得到吲哚羧酸酯(VII),其中R是指直链或支链的C1-C4烷基; f)将化合物(VII)的2-羰基烷氧基皂化,得到吲哚羧酸(VIII); g)吲哚羧酸(VIII)的脱羧,以提供佐米曲普坦,并最终提供其药学上可接受的盐。

著录项

  • 公开/公告号DE60307109T2

    专利类型

  • 公开/公告日2007-02-15

    原文格式PDF

  • 申请/专利权人

    申请/专利号DE2003607109T

  • 发明设计人

    申请日2003-08-05

  • 分类号C07D413/12;C07D413/06;C07D491/04;

  • 国家 DE

  • 入库时间 2022-08-21 20:27:44

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