公开(公告)号：US07459550B2

公开(公告)日：2008-12-02

申请号：US10563371

申请日：2004-07-03

申请人： Kumar Sahoo Prabhat ,  Anandam Vempali ,  Sivakumaran Sundaravadivelan ,  Nagesh Ganesh Praveen ,  Manikrao Waghdare Vittal ,  Balawant Deshpande Pandurang ,  Kumar Luthra Parven ,  Ramesh Sathe Pratik

发明人： Kumar Sahoo Prabhat ,  Anandam Vempali ,  Sivakumaran Sundaravadivelan ,  Nagesh Ganesh Praveen ,  Manikrao Waghdare Vittal ,  Balawant Deshpande Pandurang ,  Kumar Luthra Parven ,  Ramesh Sathe Pratik

IPC分类号： C07D501/24

CPC分类号： C07D501/04

摘要： The present invention relates to an improved process for the preparation of Cefditoren of formula (I), the said process comprising the steps of: i) converting the compound of formula (II) to a compound of the formula (III) using TPP and sodium iodide in the presence of THF, water, and base; ii) reacting the compound of formula (III) with 4-methyl-5-formyl-thiazole to produce a compound of formula (IV); iii) deesterifying the compound of the formula (IV) to yield compound of formula (V); iv) converting the compound of formula (V) to compound of formula (VI) in the presence of a base and solvent; v) converting the compound of formula (VI) into compound of formula (VII) by enzymatic hydrolysis; and vi) reacting compound of formula (VII) with compound of formula (VIII) in the presence of solvent and base to produce compound of formula (I).

摘要翻译： 本发明涉及制备式（I）的头孢托仑的改进方法，所述方法包括以下步骤：i）使用TPP和钠将式（II）化合物转化为式（III）化合物 碘化物在THF，水和碱的存在下反应; ii）使式（III）化合物与4-甲基-5-甲酰基 - 噻唑反应以制备式（IV）化合物; iii）将式（Ⅳ）化合物酯化，得到式（Ⅴ）化合物; iv）在碱和溶剂的存在下将式（Ⅴ）化合物转化成式（Ⅵ）化合物; v）通过酶水解将式（Ⅵ）化合物转化成式（Ⅶ）化合物; 和vi）使式（VII）的化合物与式（VIII）的化合物在溶剂和碱的存在下反应，得到式（I）的化合物。