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    Process for bicyclic beta-lactams
    32.
    发明公开
    Process for bicyclic beta-lactams 失效
    Herstellung von bizyklischen beta-Laktamen的Verfahrenfür

    公开(公告)号：EP0460881A1

    公开(公告)日：1991-12-11

    申请号：EP91304975.5

    申请日：1991-06-03

    申请人： THE UNIVERSITY OF NOTRE DAME DU LAC

    发明人： Miller, Marvin Joseph ,  Williams, Matthew Alan

    IPC分类号： C07D463/00 ,  C07D477/00 ,  C07D205/08 ,  C07D205/085

    CPC分类号： C07D477/04 ,  C07D463/04

    摘要： 1-Carbapenam-2-one-3-carboxylic acid and 1-carba-3-hydroxy-3-cephem-4-carboxylic acid and esters thereof are provided by a process comprising a rhodium C₂-C₁₀ carboxylate catalyzed cyclization of an ester of a 4-(1-alkoxy- or 1-substituted alkoxy)-2-oxo-4-azetidinyl)-α-diazo-β-ketobutyric acid and an ester of a 5-(1-alkoxy- or 1-substituted alkoxy-2-oxo-4-azetidinyl)-α-diazo-β-ketovaleric acid respectively. The process is carried out in an inert organic solvent at a temperature between about 15° C and about 85° C. The 1-carba bicyclic β-lactams are intermediates for preparing antibiotics.

    摘要翻译： 1-碳青霉烯-2-酮-3-羧酸和1-咔唑-3-羟基-3-头孢烯-4-羧酸及其酯通过包括铑C2-C10羧酸酯催化环化的方法提供， 4-（1-烷氧基 - 或1-取代的烷氧基）-2-氧代-4-氮杂环丁烷基）-α-重氮-β-酮丁酸和5-（1-烷氧基 - 或1-取代的烷氧基 - 2-氧代-4-氮杂环丁烷基）-α-重氮-β-酮戊酸。 该方法在约15℃至约85℃的温度下在惰性有机溶剂中进行.1-碳双环β-内酰胺是制备抗生素的中间体。

    Cephalosporinderivatives, process for their preparation and pharmaceutical compositions
    33.
    发明公开
    Cephalosporinderivatives, process for their preparation and pharmaceutical compositions 失效
    Cephalosporinverbindungen，Verfahren zu ihrer Herstellung und pharmazeutischePräparate。

    公开(公告)号：EP0418020A2

    公开(公告)日：1991-03-20

    申请号：EP90309901.8

    申请日：1990-09-10

    申请人： BEECHAM GROUP PLC

    发明人： Gasson, Brian Charles ,  Hinks, Jeremy David

    IPC分类号： C07D501/36 ,  C07D501/46 ,  C07D501/59 ,  A61K31/545 ,  C07D463/00 ,  C07D498/053 ,  C07D501/18

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： β-Lactam compounds of the formula (I) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics:
    wherein



    R 1 is hydrogen, methoxy or formamido;
    R 2 is an acyl group, in particular that of an antibacterially active cephalosporin;
    R 3 is hydrogen or a readily removable carboxy protecting group (such as a pharmaceutically acceptable in-vivo hydrolysable ester group);
    R 4 is a y- or δ-lactone,ring optionally containing one or (where applicable) two endocyclic double bonds, which ring is optionally substituted at any carbon atom by alkyl, dialkylamino, alkoxy, hydroxy, halogen or aryl, which in the case of more than one substituent may be the same or different, or is optionally di-substituted at two adjacent carbon atoms, which are available for substitution, to form an aromatic fused bicyclic system; x and y are independently 0 or 1; x is S, SO, S0 2 , 0 or CH 2 ; and Y is 0 or S.

    摘要翻译： 式（I）的β-内酰胺化合物包括药学上可接受的盐和体内可水解的酯，其制备方法及其作为抗生素的用途：其中R 1是氢，甲氧基或甲酰氨基; R 2是酰基，特别是抗菌活性头孢菌素的酰基; R 3是氢或易除去的羧基保护基（例如药学上可接受的体内可水解的酯基）; R 4是γ-或δ-内酯，任选地含有一个或（如适用的话）两个内环双键，所述环在任何碳原子上被烷基，二烷基氨基，烷氧基，羟基，卤素或芳基任选取代， 在多于一个取代基的情况下可以相同或不同，或者在可用于取代的两个相邻碳原子处任意地被二取代，以形成芳族稠合双环体系; x和y独立地为0或1; x是S，SO，SO 2，O或CH 2; 而Y是O或S.

    Solvates of a beta-lactam antibiotic
    34.
    发明公开
    Solvates of a beta-lactam antibiotic 失效
    溶剂化β-内酰胺 - 抗生素。

    公开(公告)号：EP0369687A1

    公开(公告)日：1990-05-23

    申请号：EP89311637.6

    申请日：1989-11-10

    申请人： ELI LILLY AND COMPANY

    发明人： Eckrich, Thomas Michael ,  Hoying, Richard Charles

    IPC分类号： C07D463/00

    CPC分类号： C07D463/22

    摘要： The crystalline bis(DMF), dihydrate mono(DMF) and mono(DMF) forms of 7β-[2′-(R)-2′-phenyl-2′-amino­acetamido] -3-chloro-3-(1-carbadethiacephem)-4-­carboxylic acid (LY163892) are useful intermediates to the monohydrate form of LY163892.

    摘要翻译： 7β-[2分钟 - （R）-2分钟 - 苯基-2min-氨基乙酰胺基] -3-氯-3-（1-（2-甲基苯基） 碳酸二乙酯）-4-羧酸（LY163892）是LY163892一水合物形式的有用中间体。