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NEW PROSTAGLANDIN I GROUP

机译:新前列腺素I集团

摘要

NEW MATERIAL:A prostaglandin I shown by formula I or formula II (R1 is H or alkyl; R2 and R'2 are each independently H, halogen, alkyl, aromatic group-containing group, hydroxyl group or alkoxy with the proviso that a case where R2 and R'2 are H at the same time is omitted) or a salt thereof. EXAMPLE:13,14-Dihydro-15-keto-16(RS)-fluoro-9(O)-methanol- 6(9alpha) PGI1 methyl ester. USE:Useful as an antihypertensive agent effective for alleviating other pharmaceutical and physiological action such as increase in pulse rate. PREPARATION:For example, a compound shown by formula III is reacted with an ylide prepared from (3-carboxypropyl)triphenylphosphine bromide and potassium t-butoxide, further with diazomethane to give a compound shown by formula IV. Then the compound is desilylated, subjected to Collins' oxidation, reacted with a specific anion and further reduced to give an ester derivative of a compound shown by formula I.
机译:新材料:式I或式II所示的前列腺素I(R1是H或烷基; R2和R'2各自独立地是H,卤素,烷基,含芳基的基团,羟基或烷氧基,条件是(其中R2和R'2同时为H)(或其盐)。实施例:13,14-二氢-15-酮-16(RS)-氟-9(O)-甲醇-<6(9α)> PGI1甲酯。用途:用作降压药,可有效减轻其他药物和生理作用,例如增加脉搏率。制备:例如,使式III所示的化合物与由(3-羧丙基)三苯基膦溴化物和叔丁醇钾制得的叶立德反应,再与重氮甲烷反应,得到式IV所示的化合物。然后将该化合物去甲硅烷基化,进行柯林斯氧化,与特定阴离子反应,然后进一步还原,得到式I所示化合物的酯衍生物。

著录项

  • 公开/公告号JPH02131446A

    专利类型

  • 公开/公告日1990-05-21

    原文格式PDF

  • 申请/专利权人 UENO SEIYAKU OYO KENKYUSHO:KK;

    申请/专利号JP19880286274

  • 发明设计人 UENO RYUZO;UENO TAKASHI;ODA TOMIO;

    申请日1988-11-10

  • 分类号A61K31/557;A61P9/12;C07C59/90;C07C69/738;C07C405/00;

  • 国家 JP

  • 入库时间 2022-08-22 06:26:25

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