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    • 2. 发明申请
    • Process for the manufacture of cefpodoxime proxetil
    • 头孢泊肟酯的制备方法
    • US20060149055A1
    • 2006-07-06
    • US10541473
    • 2003-01-06
    • Milind GharpureSanjay DeshmukhRajendra Mahale
    • Milind GharpureSanjay DeshmukhRajendra Mahale
    • C07D501/14
    • C07D501/60C07D501/04C07D501/12
    • A process for obtaining cefpodoxime proxetil of formula (I), of high purity conforming to pharmacopoeial specifications is disclosed. The process comprises addition of a solution of methanesulfonic acid in water to a solution of impure cefpodoxime proxetil of formula (I) in an organic solvent to form the corresponding cefpodoxime proxetil methanesulfonate of formula (II1), followed by addition of a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II1) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II1) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6, or, addition of impure cefpodoxime proxetil of formula (I) to a solution of methanesulfonic acid in water to form the corresponding solution of cefpodoxime proxetil methanesulfonate of formula (II1) in water, followed by sequential addition of a first organic solvent and a co-solvent and separation of the aqueous phase containing cefpodoxime proxetil methanesulfonate of formula (II1) having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6 and subsequent neutralization of the methaneulfonate salt (II1) with a base to give cefpodoxime proxetil (I) free of impurities and having a diastereomeric ratio of (R/R+S) between 0.5 to 0.6.
    • 公开了一种获得符合药典规格的高纯度的式(I)头孢泊肟酯的方法。 该方法包括将甲磺酸水溶液加入到有机溶剂中的式(I)不纯的头孢泊肟酯的溶液中以形成相应的式(II)的头孢泊肟甲磺酸盐,随后 通过加入共溶剂和含有非对映异构体比率为(R / R + S)为0.5至0.6的式(II-1)的头孢泊肟甲基磺酸酯的水相的分离,随后中和 具有碱的甲磺酸盐(II-1),得到不含杂质并且(R / R + S)的非对映异构体比率在0.5至0.6之间的头孢泊肟酯(I),或加入不纯 式(I)的头孢泊肟酯与甲磺酸在水中的溶液形成相应的式(II 1)的头孢泊肟甲磺酸盐溶液在水中的溶液,然后依次加入第一有机溶剂和 共溶剂和水相c的分离 使用具有(R / R + S)的非对映异构体比率为0.5至0.6的随后的甲磺酸盐中和的式(II-1)的头孢泊肟甲磺酸酯(II 1) ),得到不含杂质的头孢泊肟酯(I)和(R / R + S)的非对映异构体比例在0.5至0.6之间。