首页> 外国专利> Epinegamycin antibacterial - or 2-3R, 5S-3,6-di:amino-5-hydroxy-hexanoyl 1-methyl hydrazino-acetic acid, prepd. from protected 6-azido-3-amino-5-hydroxy-hexanoyl deriv.

Epinegamycin antibacterial - or 2-3R, 5S-3,6-di:amino-5-hydroxy-hexanoyl 1-methyl hydrazino-acetic acid, prepd. from protected 6-azido-3-amino-5-hydroxy-hexanoyl deriv.

机译:抗菌素依加霉素-或2-3R,5S-3,6-二:氨基-5-羟基-己酰基1-甲基肼基乙酸,制备。由保护的6-叠氮基-3-氨基-5-羟基-己酰基衍生而来。

摘要

Epinegamycin 2-(3R,5S-3,6-diamino-5-hydroxy-hexanoyl)-1-methyl-hydrazino-acet- ic acid of formula (II) as the racemic or optically active form with the absolute configuration (7R, 9S-correspond. to 3,5 positions of the hexanoyl radical) and its acid addn. salts are new. (II) is prepd. by catalytic hydrogenation of (III). In (III) A is an amine protecting group e.g. benzyloxycarbonyl which may be removed by hdyrogenolysis and B is an acid protecting group e.g. benzyl removal by hydrogenolysis. (II) are antibacterials effective against Gram-negative and Gram-positive organisms which may be administered orally, rectally, topically or pref. parenterally.
机译:式(II)的外来霉素2-(3R,5S-3,6-二氨基-5-羟基-己酰基)-1-甲基-肼基乙酸为外消旋或旋光形式,具有绝对构型(7R, 9S-对应于己酰基基团的3,5位及其酸加成。盐是新的。 (II)准备。 (III)的催化氢化。在(Ⅲ)中,A是一个胺保护基,例如:A。苄氧基羰基可以通过热解法除去,而B是一个酸保护基,例如B。通过氢解除去苄基。 (II)是对革兰氏阴性和革兰氏阳性生物有效的抗菌剂,可以口服,直肠,局部或优选给药。肠胃外。

著录项

  • 公开/公告号FR2433508B1

    专利类型

  • 公开/公告日1981-01-30

    原文格式PDF

  • 申请/专利权人 ICI PHARMA;

    申请/专利号FR19780024016

  • 发明设计人

    申请日1978-08-17

  • 分类号C07C109/097;A61K31/16;

  • 国家 FR

  • 入库时间 2022-08-22 15:05:41

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