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    PROCESS FOR PREPARATION OF PENAM DERIVATIVES FROM CEPHAM DERIVATIVES
    5.
    发明申请
    PROCESS FOR PREPARATION OF PENAM DERIVATIVES FROM CEPHAM DERIVATIVES 审中-公开
    从CEPHAM衍生物制备PENAM衍生物的方法

    公开(公告)号：WO2003104241A1

    公开(公告)日：2003-12-18

    申请号：PCT/IB2002/002230

    申请日：2002-06-12

    Applicant: ORCHID CHEMICALS & PHARMACEUTICALS LIMITED ,  DESHPANDE, Pandurang, Balwant ,  SENTHILKUMAR, Udayampalayam, Palanisamy ,  ANDREW, G.

    Inventor： DESHPANDE, Pandurang, Balwant ,  SENTHILKUMAR, Udayampalayam, Palanisamy ,  ANDREW, G.

    IPC: C07D499/06

    CPC classification number: C07D499/00 ,  Y02P20/55

    Abstract: The present invention provides a novel process for preparing a 2b-heterocyclyl methyl penam derivatives of the formula (I): (I)where R1 represents hydrogen, carboxylic acid protecting group such as an ester or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, NH2, acylamino, phthalimido with a proviso that both R2 and R3 are not NH2, acylamino, phthalimido; Het represents a 5 or 6-membered NH containing heterocycle ring system containing one or more heteroatoms selected from O, S, or N, which comprises :(i) reacting a compound of formula (VII) where L represents a leaving group with a compound of formula (VIII) where Het is as defined earlier in the presence of a solvent and base at a temperature in the range of -10 to 110 °C to produce a compound of formula (IX); (ii) oxidizing the compound of formula (IX) using conventional oxidizing agents in the presence of water miscible solvent and an organic acid to produce a compound a formula (I) and if necessary; and (iii) de-esterifying the compound of formula (I) where R1 represents a carboxy protecting group to a compound of formula (I) where R1 represents hydrogen using metal catalyst, in the presence of a base and water immiscible solvent.

    Abstract translation: 本发明提供了制备式（I）的式（I）的2b-杂环基甲基对苯二胺衍生物的新方法：其中R 1表示氢，羧酸保护基如酯或药学上可接受的盐; R2和R3可以相同或不同，并且独立地代表氢，卤素，NH2，酰氨基，苯二甲酰亚氨基，条件是R2和R3都不是NH2，酰氨基，邻苯二甲酰亚氨基; Het表示含有一个或多个选自O，S或N的杂原子的5或6元含NH的杂环环系，其包含：（i）使式（Ⅶ）化合物（其中L表示离去基团）与化合物 其中Het如前所定义，在溶剂和碱的存在下，在-10至110℃的温度范围内，得到式（Ⅸ）化合物; （ii）在水混溶性溶剂和有机酸的存在下，使用常规氧化剂氧化式（IX）化合物，以产生式（I）化合物，如果需要; 和（iii）在碱和水不混溶的溶剂的存在下，使用金属催化剂将其中R 1表示羧基保护基的式（I）化合物脱羧化为式（I）化合物，其中R 1表示氢。

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