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    • 6. 发明授权
    • Process for the production of 3-vinyl cephalosporins
    • 生产3-乙烯基头孢菌素的方法
    • US06414140B2
    • 2002-07-02
    • US09792800
    • 2001-02-23
    • Josef WieserGerd AscherJohannes LudescherHerbert Sturm
    • Josef WieserGerd AscherJohannes LudescherHerbert Sturm
    • C07D50122
    • C07D501/00
    • 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.
    • 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。