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    2-Vinylpenams and process
    2.
    发明公开
    2-Vinylpenams and process 失效
    2-Vinylpenams和过程

    公开(公告)号：EP0244195A1

    公开(公告)日：1987-11-04

    申请号：EP87303725.3

    申请日：1987-04-28

    申请人： THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD

    发明人： Baldwin, Jack Edward

    IPC分类号： C12P37/00 ,  C07D499/44 ,  C07D499/42

    CPC分类号： C07D499/00 ,  C12P37/00 ,  C12R1/75

    摘要： 6β-(L-α-Aminoadipoyl)-2α-vinyl-2β-methylpenam-­3-carboxylic acid is provided in an enzymatic process converting δ-(L-α-aminoadipoyl)-L-cysteinyl-D-γ,δ-­didehydroisoleucine with isopenicillin N synthetase. The 2α-vinylpenam product is converted by known methods to the 6β-amino-2α-vinyl-2β-methylpenam-3-carboxylic acid nucleus and the latter is N-acylated to provide corresponding 6β-acylaminopenams.

    摘要翻译： 在酶促过程中提供6β-（L-α-氨基己二酰）-2α-乙烯基-2β-甲基戊烷-3-羧酸，将δ-（L-α-氨基己二酰）-L-半胱氨酰-D-γ，δ-双脱氢异亮氨酸 与异青霉素N合成酶。 通过已知方法将2α-乙烯基铁蛋白产物转化为6β-氨基-2α-乙烯基-2β-甲基戊-3-羧酸核，后者N-酰化以提供相应的6β-酰氨基苯丙氨酸。

    Process for preparing penicillin and cephalosporin sulfones
    5.
    发明公开
    Process for preparing penicillin and cephalosporin sulfones 失效
    Verfahren zur Herstellung von青霉素和头孢菌素磺隆。

    公开(公告)号：EP0136788A1

    公开(公告)日：1985-04-10

    申请号：EP84305359.6

    申请日：1984-08-07

    申请人： ELI LILLY AND COMPANY

    发明人： Hatfield, Lowell Deloss

    IPC分类号： C07D499/04 ,  C07D501/04 ,  C07D499/44 ,  C07D501/20

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： There is disclosed a process for preparing a penicillin or cephalosporin sulfone of the formula

    wherein:

    R' is hydrogen or a carboxylic acid acyl residue;
    R 2 is hydrogen or lower alkoxy;
    R 3 is hydrogen, a carboxy protecting group or a salt forming group;
    A is

    in which:
    R 4 is halo, lower alkyl, lower alkoxy, or -CH 2 R 6 , wherein R 6 is lower alkanoyloxy or a heterocyclic group; and
    R 5 is hydrogen or alkoxycarbonyloxy; comprising reacting a compound of the formula
    with an oxidizing agent and a catalytic amount of ruthenium tetroxide.

    摘要翻译： 公开了一种制备下式的青霉素或头孢菌素砜的方法：其中：R 1是氢或羧酸酰基残基; R 2是氢或低级烷氧基; 其中：R 4是卤素，低级烷基，低级烷氧基或-CH 2 R 6，其中R 3是氢，羧基保护基或成盐基; A是... 6>是低级烷酰氧基或杂环基; 和R 5是氢或烷氧基羰基氧基; 包括使式...的化合物与氧化剂和催化量的四氧化钌反应。

    Process for preparing 2-alpha-methyl-2-beta-(1,2,3-triazol-1-yl)methyl-penam-3-alpha-carboxylic acid derivatives
    9.
    发明公开
    Process for preparing 2-alpha-methyl-2-beta-(1,2,3-triazol-1-yl)methyl-penam-3-alpha-carboxylic acid derivatives 失效
    Verfahren zur Herstellung von 2-α-Methyl-2-β-（1,2,3-三唑-1-基）甲基扑灭-3-α-碳二烯酸酯。

    公开(公告)号：EP0331395A1

    公开(公告)日：1989-09-06

    申请号：EP89301926.5

    申请日：1989-02-27

    申请人： TAIHO PHARMACEUTICAL COMPANY LIMITED ,  OTSUKA KAGAKU KABUSHIKI KAISHA

    发明人： Torii, Sigeru ,  Tanaka, Hideo ,  Tanaka, Motoaki ,  Yamada, Shozo ,  Nakai, Akira

    IPC分类号： C07D499/00 ,  C07D499/44

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： 2α-Methyl-2β-(1,2,3-triazol-1-yl)methylpenam-3α-­carboxylic acid derivatives are prepared by reacting a penicillanic acid sulfoxide derivative of the formula
    wherein R is a penicillin carboxyl protecting group, and R₁ is hydrogen or halogen, R₂ is hydrogen, lower alkyl or the like with a triazole derivative of the formula
    wherein R₃ and R₄ are hydrogen, trialkylsilyl, lower alkyl, lower alkoxy or the like and R₅ is hydrogen or silyl substituted with 3 groups selected from the class consisting of lower alkyl, benzyl and phenyl in a solvent.

    摘要翻译： 2α-甲基-2β-（1,2,3-三唑-1-基）甲基亚磺酸-3α-羧酸衍生物通过使式的青霉烷酸亚砜衍生物，其中R是青霉素羧基 R 1为氢或卤素，R 2为氢，低级烷基等与式CHEM的三唑衍生物反应，其中R 3和R 4为氢，三烷基甲硅烷基，低级烷基，低级烷氧基等，R 5为氢 或在溶剂中由选自低级烷基，苄基和苯基的3种基团取代的甲硅烷基。