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    Novel Method for the Preparation of Aryl Piperazinyl-Heterocyclic Compounds
    3.
    发明申请
    Novel Method for the Preparation of Aryl Piperazinyl-Heterocyclic Compounds 失效
    芳基哌嗪基杂环化合物的制备方法

    公开(公告)号：US20070238877A1

    公开(公告)日：2007-10-11

    申请号：US11630054

    申请日：2005-06-16

    申请人： Om Tyagi ,  Tushar Srivastava ,  Yogendra Chauhan ,  Vasanth Nalam

    发明人： Om Tyagi ,  Tushar Srivastava ,  Yogendra Chauhan ,  Vasanth Nalam

    IPC分类号： C07D417/14

    CPC分类号： C07D417/12

    摘要： A novel method for preparing a compound of formula I which comprises of coupling the piperazine derivative of formula II with alkyl halide containing compound of the formula III by heating in solvent free conditions or, optionally, in a minimum quantity of non-aqueous suspending liquid, in presence of a catalyst and a neutralizing agent to neutralize the hydrohalic acid.

    摘要翻译： 一种制备式I化合物的新方法，其包括将式II的哌嗪衍生物与含有式III的化合物的烷基卤化合物在无溶剂条件下加热，或任选地在最少量的非水性悬浮液中偶联， 在催化剂和中和剂存在下中和氢卤酸。

    Process for preparation of 7-[a-amino (4-hydroxyphenyl) acetamido]-3-substituted-3-cephem-4-carboxylic acid
    4.
    发明申请
    Process for preparation of 7-[a-amino (4-hydroxyphenyl) acetamido]-3-substituted-3-cephem-4-carboxylic acid 有权
    制备7- [α-氨基（4-羟基苯基）乙酰氨基] -3-取代-3-头孢烯-4-羧酸的方法

    公开(公告)号：US20060149096A1

    公开(公告)日：2006-07-06

    申请号：US11360283

    申请日：2006-02-23

    申请人： Om Tyagi ,  Dnyandev Rane ,  Tushar Srivastava ,  Krishnarao Sirsath

    发明人： Om Tyagi ,  Dnyandev Rane ,  Tushar Srivastava ,  Krishnarao Sirsath

    IPC分类号： C07C227/06

    CPC分类号： C07D501/00 ,  C07C229/34 ,  C07F7/1804

    摘要： A process for preparation of 7-[D-α-amino-α-(4-hydroxyphenyl)acetamido]-3-(1-propen-1-yl)-3-cepham-4-carboxylic acid viz. Cefprozil of formula (I) igh purity, substantially free of impurities, which comprises preparation of mixed acid anhydride by selecting the sequence and temperature of addition of the reagents and its subsequent condensation with a protected 7-APCA; followed by hydrolysis, isolation and purification to give Cefprozil of formula (I) in the form of a monohydrate.

    摘要翻译： 制备7- [D-α-氨基-α-（4-羟基苯基）乙酰氨基] -3-（1-丙烯-1-基）-3-头孢烯-4-羧酸的方法， 式（I）的头孢夫唑高纯度，基本上不含杂质，其包括通过选择试剂的加入顺序和温度及其随后与受保护的7-APCA的缩合制备混合酸酐; 然后水解，分离和纯化，得到一水合物形式的式（I）的头孢普利。

    Method for manufacture of ceftiofur
    5.
    发明申请
    Method for manufacture of ceftiofur 失效
    头孢噻呋的制造方法

    公开(公告)号：US20060149054A1

    公开(公告)日：2006-07-06

    申请号：US10532194

    申请日：2003-10-27

    申请人： Om Tyagi ,  Santosh Richhariya ,  Rajesh Pawar ,  Yuvaraj Chavan

    发明人： Om Tyagi ,  Santosh Richhariya ,  Rajesh Pawar ,  Yuvaraj Chavan

    IPC分类号： C07D501/14

    CPC分类号： C07D417/14

    摘要： A process for preparation of ceftiofur of formula (I) of high purity and substantially free from impurities is disclosed. The process comprises reacting [2-(2-aminothiazol-4-yl)]-2-syn-methoxyimino acetic acid-2-benzothiazolyl thioester of formula (II), with 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid of formula (III) in the presence of a mixture of an water-immescible inert organic solvent and water and in the presence of a organic base and isolating ceftiofur of formula (I) substantially free of impurities by, d) adding water to the reaction mixture and selectively partitioning the impurities in the organic phase and ceftiofur (I) in the form of a salt with the base in the aqueous phase, e) acidifying the aqueous phase containing ceftiofur (I) in the form of a salt with the base in the presence of a mixture containing a water-miscible and a water-immiscible organic solvent and in the presence of a saturated aqueous solution of an alkali or alkaline earth containing salt, to partition ceftiofur (I) in the organic phase, and f) isolating ceftiofur (I) of high purity and substantially free of impurities by evaporation of the organic solvent or precipitation by addition of a co-solvent.

    摘要翻译： 公开了一种制备高纯度且基本上不含杂质的式（I）头孢噻呋的方法。 该方法包括使式（II）的[2-（2-氨基噻唑-4-基）] - 2-顺式 - 甲氧基亚氨基乙酸-2-苯并噻唑基硫代酯与7-氨基-3-（2-呋喃基羰硫基甲基）-3 （III）的头孢-4-羧酸在水不溶性惰性有机溶剂和水的混合物存在下，在有机碱的存在下，分离基本上不含杂质的式（I）头孢噻呋， d）向反应混合物中加入水，并在水相中选择性地分配有机相中的杂质和与碱的盐形式的头孢噻呋（I），e）以含有头孢噻呋（I）的形式酸化含有头孢噻呋 在含有水混溶性和与水不混溶的有机溶剂的混合物存在下，在含有碱或碱土金属盐的饱和水溶液的存在下，将碱与碱反应，从而将头孢噻吩（I） 有机相，和f）分离高纯度和实质的头孢噻呋（I） 通过蒸发有机溶剂或通过加入共溶剂沉淀而不含杂质。