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    Oxidation Process For Preparing 3-Formyl-Cephem Derivatives
    4.
    发明申请
    Oxidation Process For Preparing 3-Formyl-Cephem Derivatives 有权
    用于制备3-甲酰基头孢烯衍生物的氧化方法

    公开(公告)号：US20150218189A1

    公开(公告)日：2015-08-06

    申请号：US14680548

    申请日：2015-04-07

    申请人： Basilea Pharmaceutica International

    发明人： Ivan Joseph Maria Vervest

    IPC分类号： C07D501/04

    CPC分类号： C07D501/04 ,  C07D501/34

    摘要： The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.

    摘要翻译： 本发明涉及将3-羟基甲基头孢烯衍生物氧化为相应的3-甲酰基头孢烯衍生物的改进方法。 特别地，该氧化方法用于制备7- [2-（5-氨基 - [1,2,4]噻二唑-3-基）-2-羟基亚氨基 - 乙酰基氨基] -3-甲酰基-8-氧代 -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸衍生物，其使用10-I-3型的高价碘氧化剂的组合，例如 双（乙酰氧基）碘 - 苯（BAIB）和催化剂如2,2,6,6-四甲基-1-哌啶氧基（TEMPO）。 这些式（I）化合物是合成头孢匹罗的中间体。

    Methods and compounds for detecting beta-lactamase activity
    6.
    发明授权
    Methods and compounds for detecting beta-lactamase activity 有权
    检测β-内酰胺酶活性的方法和化合物

    公开(公告)号：US08802387B2

    公开(公告)日：2014-08-12

    申请号：US12113109

    申请日：2008-04-30

    申请人： Bengang Xing ,  Xianfeng Huang ,  Tingting Jiang ,  Rongrong Liu

    发明人： Bengang Xing ,  Xianfeng Huang ,  Tingting Jiang ,  Rongrong Liu

    IPC分类号： C12Q1/34 ,  C07D501/00

    CPC分类号： C12Q1/34 ,  C07D501/04 ,  C07D501/16 ,  C07D501/18 ,  C07D519/06 ,  G01N2333/986

    摘要： The present invention relates to compounds for and a method of detecting beta-lactamase activity in a sample. The sample is contacted with a nanoparticulate tag. The nanoparticulate tag comprises a metal or a combination of metals, or it comprises a nanotube of a metal, boron nitride and/or carbon. The respective metal is capable of forming one of a covalent bond, a coordinative bond and a non-covalent interaction with a thio or a seleno group. The sample is contacted with a compound of one of general formulas (I)-(III) and (VII)-(IX). At least one beta-lactam moiety of the compound is cleaved by the beta-lactamase activity in the sample. As a result a cleavage moiety Z-A-Z, Z-A-Z—R15, Z-A-Z—R16, Z-A-Z—R17, Z-A-Z—R18 or Z-G-N(R8)R9 is released that is immobilised on the surface of the nanoparticulate tag by a covalent bond via a Z atom. The presence of beta-lactamase activity is determined based on the presence of the cleavage moiety immobilized onto the surface of the nanoparticulate tag.

    摘要翻译： 本发明涉及用于检测样品中β-内酰胺酶活性的化合物和方法。 样品与纳米颗粒标签接触。 纳米颗粒标签包括金属或金属的组合，或者它包括金属，氮化硼和/或碳的纳米管。 相应的金属能够形成共价键，配位键和与硫代或硒基的非共价相互作用之一。 将样品与通式（I） - （III）和（VII） - （IX）之一的化合物接触。 化合物的至少一个β-内酰胺部分被样品中的β-内酰胺酶活性切割。 结果，通过Z原子通过共价键将解离部分Z-A-Z，Z-A-Z-R15，Z-A-Z-R16，Z-A-Z-R17，Z-A-Z-R18或Z-G-N（R8）R9释放固定在纳米颗粒标签的表面上。 基于固定在纳米颗粒标签表面上的切割部分的存在来确定β-内酰胺酶活性的存在。

    Process for the preparation of Cefditoren
    7.
    发明授权
    Process for the preparation of Cefditoren 失效
    头孢托仑的制备方法

    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。

    7-(S)-Acylaminocephalosporin sulfones and process
    10.
    发明授权
    7-(S)-Acylaminocephalosporin sulfones and process 失效
    7-（S） - 氨基头孢菌素砜及方法

    公开(公告)号：US4477660A

    公开(公告)日：1984-10-16

    申请号：US442077

    申请日：1982-11-16

    申请人： David A. Hall

    发明人： David A. Hall

    IPC分类号： C07D20060101 ,  C07D501/04 ,  C07D501/20 ,  C07D501/26 ,  C07D501/32

    CPC分类号： C07D501/04 ,  C07D501/26

    摘要： This invention encompasses 7-(S)-acylamino-3-acetoxymethyl-3-cephem-4-carboxylic acid sulfones and the epimerization process for making them. The epimerization process employs an organic nitrogen base reagent having a pKa between about 9.0 to about 11.5. The compounds of this invention are intermediates in the synthesis of 1-oxa-.beta.-lactam antibiotics.

    摘要翻译： 本发明包括7-（S） - 酰基氨基-3-乙酰氧基甲基-3-头孢烯-4-羧酸砜和用于制备它们的差向异构化方法。 差向异构化方法使用pKa在约9.0至约11.5之间的有机氮碱试剂。 本发明的化合物是合成1-氧代-β-内酰胺抗生素的中间体。