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    Process for synthesis of azetidinones
    231.
    发明专利
    Process for synthesis of azetidinones 审中-公开
    合成AZETIDINONES的方法

    公开(公告)号：JP2012036224A

    公开(公告)日：2012-02-23

    申请号：JP2011252865

    申请日：2011-11-18

    Applicant: Schering Corp ,  シェーリング コーポレイションSchering Corporation

    Inventor： THIRUVETTIPURAM THIRUVENGADAM K ,  CHIU JOHN S ,  FU XIAOYONG ,  MCALLISTER TIMOTHY L

    IPC: C07D205/08 ,  C07D201/02

    CPC classification number: C07D205/08 ,  C07H17/02

    Abstract: PROBLEM TO BE SOLVED: To provide a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents.SOLUTION: The process includes reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent. The cyclizing agent is selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride.

    Abstract translation: 要解决的问题：提供一种制备可用作半乳聚糖和低胆固醇血症药的中间体的氮杂环丁酮的方法。 解决方案：该方法包括使β-（取代氨基）酰胺，β-（取代氨基）酸酯或β-（取代氨基）硫代碳酸酯与甲硅烷基化剂和环化剂 。 环化剂选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵芳氧化物及其水合物，或其反应产物：（i）至少一种季铵卤化物和 至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物。 版权所有（C）2012，JPO＆INPIT

    METHOD FOR PRODUCING ε-CAPROLACTAM
    233.
    发明专利
    METHOD FOR PRODUCING ε-CAPROLACTAM 有权
    生产ε-CAPROLACTAM的方法

    公开(公告)号：JP2007262037A

    公开(公告)日：2007-10-11

    申请号：JP2006092871

    申请日：2006-03-30

    Applicant: Ube Ind Ltd ,  宇部興産株式会社

    Inventor： KUGIMOTO JUNICHI

    IPC: C07C45/53 ,  C07B61/00 ,  C07C49/403 ,  C07D201/02

    CPC classification number: Y02P20/52 ,  Y02P20/584

    Abstract: PROBLEM TO BE SOLVED: To provide a method for producing ε-caprolactam and cyclohexanone in a high selectivity by decomposing 1,1'-peroxydicyclohexylamine selectively, also reduce the using amount of the catalyst by reducing a catalyst concentration and/or performing the recycle of the catalyst. SOLUTION: This method for producing ε-caprolactam and cyclohexanone is characterized by decomposing 1,1'-peroxydicyclohexylamine by using a catalyst of a lithium salt and an adduct consisting of an amide having a higher nucleophilicity than that of ε-caprolactam and a lower nucleophilicity than that of 1,1'-peroxydicyclohexylamine. COPYRIGHT: (C)2008,JPO&INPIT

    Abstract translation: 待解决的问题：为了通过选择性地分解1,1'-过氧二环己基胺来提供高选择性的ε-己内酰胺和环己酮的制造方法，还可以通过降低催化剂浓度和/或进行催化剂浓度来降低催化剂的使用量 催化剂的循环。 解决方案：用于制备ε-己内酰胺和环己酮的方法的特征在于通过使用锂盐的催化剂和由具有比ε-己内酰胺更高的亲核性的酰胺组成的加合物来分解1,1'-过氧二环己基胺， 比1,1'-过氧二环己胺的亲核性低。 版权所有（C）2008，JPO＆INPIT

    3-BROMO- AND 3,3-DIBROMO-4-OXOAZETIDINE DERIVATIVES, THEIR PRODUCTION AND THEIR USE
    240.
    发明专利
    3-BROMO- AND 3,3-DIBROMO-4-OXOAZETIDINE DERIVATIVES, THEIR PRODUCTION AND THEIR USE 失效

    公开(公告)号：JPH07149716A

    公开(公告)日：1995-06-13

    申请号：JP15454694

    申请日：1994-07-06

    Applicant: PLIVA PHARM & CHEM WORKS

    Inventor： LUKIC IRENA

    IPC: A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  A61P35/00 ,  C07D201/02 ,  C07D205/08

    Abstract: The invention relates to novel 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof. According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.0/non-5-ene) and then the obtained DBN salt of sulfinic acid or isolated sulfinic acid is treated with thionyl chloride and, after eliminating thionyl chloride by evaporation, the obtained residue is passed through a silica gel column with methylene chloride or some other solvent as eluant or the obtained residue is dissolved in tetrahydrofuran or some other suitable solvent and treated with tetrabutyl ammonium, bromide and after the treatment a derivative of 2-bromo, 3-bromo or 2-bromo-3,3-dibromo-4-oxo-azetidine is isolated, which derivative may be subjected to a reaction with silver nitrate in 2-propanol and, after the treatment of the reaction mixture, derivatives of 2-nitroxy-, 3-bromo- or 2-nitroxy-3,3-dibromo-4-oxo-azetidine are isolated. The obtained substances are useful intermediates in the syntheses of beta lactam analogons or as components in formulations having antibacterial, inhibitory, anti-tumour or antagonistic action.

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