Process for the production of 3-vinyl cephalosporins
    10.
    发明授权
    Process for the production of 3-vinyl cephalosporins 失效
    生产3-乙烯基头孢菌素的方法

    公开(公告)号:US06414140B2

    公开(公告)日:2002-07-02

    申请号:US09792800

    申请日:2001-02-23

    IPC分类号: C07D50122

    CPC分类号: C07D501/00

    摘要: A process for the production of a 3-vinylcephalosporin compound of formula I wherein R1 and R2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula II with a compound of formula P(R4)3 or P(OR4)3 to produce a compound of formula III and secondly reacting the compound of formula III with a weak base of formula or of formula R10—COO−W+ wherein R5 is hydrogen, alkly or aryl and R6 and R7 are each an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2; or R5 and R8 are each aryl and R7 is an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2, W+ is an alkali metal cation and R10 is alkyl or aryl to produce a compound of formula IV and finally reacting a compound of formula IV with a compound of formula V to produce a compound of formula I.

    摘要翻译: 制备式I的3-乙酰头孢菌素化合物的方法,其中R1和R2通过维蒂希反应表示氢或有机基团,首先将式II化合物与式P(R4)3或P(OR4)3的化合物反应至 制备式III化合物,其次使式III化合物与式R 10 -COO-W +的弱碱反应,其中R 5是氢,烷基或芳基,R 6和R 7各自是式-COOR 8,-CN的活化基团 ,-SO 2 R 8,-COR 8或-CON(R 8)2; 或R 5和R 8各自为芳基,R 7为式-COOR 8,-CN,-SO 2 R 8,-COR 8或-CON(R 8)2的活化基团,W +为碱金属阳离子,R 10为烷基或芳基, 然后最终使式Ⅳ化合物与式Ⅴ化合物反应,生成式Ⅰ化合物。