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    Process for the preparation of 3-methylcepham derivatives
    3.
    发明申请
    Process for the preparation of 3-methylcepham derivatives 有权
    3-甲基头孢衍生物的制备方法

    公开(公告)号：US20050070705A1

    公开(公告)日：2005-03-31

    申请号：US10922992

    申请日：2004-08-23

    申请人： Pandurang Deshpande ,  Udayampalayam Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

    发明人： Pandurang Deshpande ,  Udayampalayam Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

    IPC分类号： C07D499/00 ,  C07D501/00

    CPC分类号： C07D501/00 ,  C07D499/00

    摘要： A process for the preparation of 3-methylcepham-4-carboxylate of the formula (I). wherein R2 and R3 may be same or different and represent hydrogen, halogen, amino, alkyl, phenacetamido, substituted acetamido, phthalimido with a proviso that both R2 and R3 are not NH2, phenacetamido, phthalimido and the like; R1 represents a lower alkyl, p-methoxybenzyl, p-nitrobenzyl, o-nitrobenzyl, o-methoxybenzyl, o-chlorobenzyl or diphenylmethyl group, or a suitable ester residue which can be deprotected at a latter stage, L represents a leaving group; which comprises cyclizing the compound of formula (III) using a cyclizing agent in the presence of organic or inorganic nitrites and a solvent at a temperature in the range of −40° C. to +60° C. to obtain compound of formula (I).

    摘要翻译： 制备式（I）的3-甲基头孢-4-羧酸酯的方法。 其中R 2和R 3可以相同或不同，表示氢，卤素，氨基，烷基，苯乙酰氨基，取代的乙酰氨基，苯二甲酰亚氨基，条件是R 2和R 3都不是NH 2，苯乙酰胺基 ，苯二甲酰亚氨基等; R1表示低级烷基，对甲氧基苄基，对硝基苄基，邻硝基苄基，邻甲氧基苄基，邻氯苄基或二苯基甲基，或可在后期脱保护的合适的酯残基，L表示离去基团; 其包括在有机或无机亚硝酸盐和溶剂的存在下，在-40℃至+ 60℃的温度下，使用环化剂环化式（III）的化合物，得到式（I ）。

    Process for the preparation of 3-methylcepham derivatives
    5.
    发明授权
    Process for the preparation of 3-methylcepham derivatives 有权
    3-甲基头孢衍生物的制备方法

    公开(公告)号：US07273935B2

    公开(公告)日：2007-09-25

    申请号：US10922992

    申请日：2004-08-23

    申请人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

    发明人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

    IPC分类号： C07D501/08 ,  C07D499/063

    CPC分类号： C07D501/00 ,  C07D499/00

    摘要： A process for the preparation of 3-methylcepham-4-carboxylate of the formula (I). wherein R2 and R3 may be same or different and represent hydrogen, halogen, amino, alkyl, phenacetamido, substituted acetamido, phthalimido with a proviso that both R2 and R3 are not NH2, phenacetamido, phthalimido and the like; R1 represents a lower alkyl, p-methoxybenzyl, p-nitrobenzyl, o-nitrobenzyl, o-methoxybenzyl, o-chlorobenzyl or diphenylmethyl group, or a suitable ester residue which can be deprotected at a latter stage, L represents a leaving group; which comprises cyclizing the compound of formula (III) using a cyclizing agent in the presence of organic or inorganic nitrites and a solvent at a temperature in the range of −40° C. to +60° C. to obtain compound of formula (I).

    摘要翻译： 制备式（I）的3-甲基头孢-4-羧酸酯的方法。 其中R 2和R 3可以相同或不同，表示氢，卤素，氨基，烷基，苯乙酰氨基，取代的乙酰氨基，苯二甲酰亚氨基，条件是R“ 2和R 3不是NH 2，苯乙酰氨基，邻苯二甲酰亚氨基等; R 1表示低级烷基，对甲氧基苄基，对硝基苄基，邻硝基苄基，邻甲氧基苄基，邻氯苄基或二苯基甲基或适合的酯残基，其可以在后一阶段脱保护 L表示离去基团; 其包括在有机或无机亚硝酸盐和溶剂的存在下，在-40℃至+ 60℃的温度下，使用环化剂环化式（III）的化合物，得到式（I ）。