Method for manufacture of ceftiofur
    1.
    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

    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。

    CRYSTALLINE FORM OF FOSAMPRENAVIR CALCIUM
    2.
    发明申请
    CRYSTALLINE FORM OF FOSAMPRENAVIR CALCIUM 审中-公开
    FOSAMPRENAVIR CALCIUM的结晶形式

    公开(公告)号:US20120208787A1

    公开(公告)日:2012-08-16

    申请号:US13379926

    申请日:2010-06-29

    摘要: The present invention relates to a crystalline form of fosamprenavir calcium. The crystalline form of the present invention is designated as Form II of fosamprenavir calcium. The present invention also relates to a process for the preparation of crystalline Form II of fosamprenavir calcium. The present invention further relates to a pharmaceutical composition comprising crystalline Form II of fosamprenavir calcium. The present invention relates further to a method of treating a HIV infection using crystalline Form II of fosamprenariv calium.

    摘要翻译: 本发明涉及福沙那韦钙的结晶形式。 本发明的结晶形式被称为福沙那韦钙的形式II。 本发明还涉及一种制备福沙那韦钙的晶型II的方法。 本发明进一步涉及一种药物组合物,其包含福沙那韦晶体钙的晶型II。 本发明进一步涉及一种使用镰刀菌镰刀菌的晶型II治疗HIV感染的方法。