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    Amides of 4-oxo-azetidine-2-sulfonic acids and salts thereof, processes for their preparation and their use
    1.
    发明授权
    Amides of 4-oxo-azetidine-2-sulfonic acids and salts thereof, processes for their preparation and their use 失效
    4-氧代 - 氮杂环丁烷-2-磺酸的酰胺及其盐，其制备及其用途

    公开(公告)号：US5466686A

    公开(公告)日：1995-11-14

    申请号：US115538

    申请日：1993-09-03

    Applicant: Mice Kovacevic ,  Jure J. Herak ,  Zora Mandic ,  Irena Lukic ,  Mirjana Tomic ,  Zinka Brkic

    Inventor： Mice Kovacevic ,  Jure J. Herak ,  Zora Mandic ,  Irena Lukic ,  Mirjana Tomic ,  Zinka Brkic

    IPC: A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  C07D205/09 ,  C07D205/095 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    CPC classification number: C07D403/12 ,  C07D205/09 ,  C07D205/095 ,  C07D413/10 ,  C07D413/14

    Abstract: The invention relates to the novel 4-oxo-azetidine-2-sulfonic acid amides and their salts of the formula I ##STR1## wherein the radicals have the meanings: R.sup.1 =hydrogen, halogen;R.sup.2 =hydrogen, halogen, NH.sub.2, C.sub.6 H.sub.5 CH.sub.2 CONH, C.sub.6 H.sub.5 OCH.sub.2 CONH, phthalimido, o-MeNHCOC.sub.6 H.sub.4 CONH, isoxazolylcarbonylamino;R.sup.3 =hydrogen, Me.sub.2 C.dbd.C--COOMe, H.sub.2 C.dbd.C(Me)--CH--COOMe, Me.sub.2 C.dbd.C--COOCH.sub.2 C.sub.6 H.sub.5, H.sub.2 C.dbd.C(Me)CH--COOCH.sub.2 C.sub.6 H.sub.4 NO.sub.2 -p, Me.sub.2 C.dbd.C--COOCH.sub.2 C.sub.6 H.sub.4 NO.sub.2 -p, Me.sub.2 C.dbd.C--COOCH.sub.2 C.sub.6 H.sub.4 Me-m, H.sub.2 C.dbd.C(Me)--CH--COOCH.sub.2 C.sub.6 H.sub.4 Me-m, Me.sub.2 C.dbd.C--COOH;R.sup.4 =hydrogen or sodium andR.sup.5 =hydrogen, alkyl, benzyl or heterocycle, i.e. isoxazole or pyrazole etc.The invention also relates to the procedure for the preparation thereof and the use thereof as intermediates in the synthesis of beta-lactam analogs or as active components for the preparations of the drugs for antimicrobial therapy.

    Abstract translation: 本发明涉及新的4-氧代 - 氮杂环丁烷-2-磺酸酰胺及其式I的盐，其中基团具有以下含义：R 1 =氢，卤素; R2 =氢，卤素，NH2，C6H5CH2CONH，C6H5OCH2CONH，苯二甲酰亚氨基，o-MeNHCOC6H4CONH，异恶唑基羰基氨基; R3 =氢，Me2C = C-COOMe，H2C = C（Me）-CH-COOMe，Me2C = C-COOCH2C6H5，H2C = C（Me）CH-COOCH2C6H4NO2-p，Me2C = C-COOCH2C6H4NO2-p，Me2C = C -COOCH 2 C 6 H 4 Me-m，H 2 C = C（Me）-CH-COOCH 2 C 6 H 4 Me-m，Me 2 C = C-COOH; R4 =氢或钠，R5 =氢，烷基，苄基或杂环，即异恶唑或吡唑等。本发明还涉及其制备方法及其作为合成β-内酰胺类似物或活性的中间体的用途 用于抗微生物治疗药物的制备成分。

    Process for the preparation of 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo-azetidines
    2.
    发明授权
    Process for the preparation of 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo-azetidines 失效
    制备3-溴 - 和3,3-二溴-4-氧代 - 氮杂环丁烷的2-溴和2-硝基氧基衍生物的方法

    公开(公告)号：US5892036A

    公开(公告)日：1999-04-06

    申请号：US926449

    申请日：1997-09-10

    Applicant: Irena Lukic

    Inventor： Irena Lukic

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

    CPC classification number: A61K31/395 ,  C07D205/08 ,  Y02P20/55

    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 lanic 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-4oxo-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.

    Abstract translation: 本发明涉及3-，溴 - 和3-二溴-4-氧代 - 氮杂环丁烷的新型2-溴 - 和2-硝基氧基衍生物，其制备方法及其用途。 根据本发明，3-溴 - 和3-二溴-4-氧代 - 氮杂环丁烷的2-溴 - 和2-硝基氧基衍生物是通过将受保护的青霉烷基酸兰酸1,1-二氧化物的衍生物与DBN反应物（1,5 - 二氮杂双环/ 3.4.0 /非-5-烯），然后将得到的亚磺酸DBI盐或分离的亚磺酸用亚硫酰氯处理，在通过蒸发除去亚硫酰氯后，将所得残余物通过硅胶柱 用二氯甲烷或一些其它溶剂作为洗脱剂，或将所得残余物溶于四氢呋喃或一些其它合适的溶剂中，并用四丁基溴化铵处理，处理后，将2-溴，3-溴或2-溴-3,3 分离出二溴-4-氧代 - 氮杂环丁烷，该衍生物可以与硝酸银在2-丙醇中进行反应，并且在处理反应混合物后，将2-硝基氧基，3-溴 - 或2-硝基氧基 - 分离出3,3-二溴-4-氧代 - 氮杂环丁烷。 获得的物质是合成β-内酰胺类似物或作为具有抗细菌，抑制，抗肿瘤或拮抗作用的制剂中的组分的有用中间体。

    5-thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo analogs of .beta.-lactam, processes for the preparation thereof and the use thereof
    3.
    发明授权
    5-thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo analogs of .beta.-lactam, processes for the preparation thereof and the use thereof 失效
    β-内酰胺的5-硫杂-1,4-二氮杂双环[4.2.0]辛烷-3,8-二氧代类似物，其制备方法及其用途

    公开(公告)号：US5446038A

    公开(公告)日：1995-08-29

    申请号：US151673

    申请日：1993-11-12

    Applicant: Mice Kovacevic ,  Jure J. Herak ,  Zora Mandiec ,  Irena Lukic ,  Mirjana Tomic ,  Zinka Brkic

    Inventor： Mice Kovacevic ,  Jure J. Herak ,  Zora Mandiec ,  Irena Lukic ,  Mirjana Tomic ,  Zinka Brkic

    IPC: A61K31/54 ,  A61K31/542 ,  A61P31/04 ,  C07D513/04

    CPC classification number: C07D513/04

    Abstract: 5-Thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo analogs of .beta.-lactam, processes for the preparation thereof and the use thereofDisclosed are novel 5-thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo .beta.-lactam analogs of the general formula I ##STR1## wherein R.sup.1 is hydrogen or halo;R.sup.2 is hydrogen, halo, amino, PhCH.sub.2 CONH, PhOCH.sub.2 CONH, phthalimido, o-MeNHCO-C.sub.6 H.sub.4 -CONH, isoxazolylcarboxamido;R.sup.3 is hydrogen, alkyl, benzyl, heterocycle, e.g. isoxazole, pyrazole etc., andn may be 1 or 2.They may be used as intermediates in preparing novel .beta.-lactam analogs or as active substances in formulations for antimicrobial therapy.

    Abstract translation: β-内酰胺的5-硫杂-1,4-二氮杂双环[4.2.0]辛烷-3,8-二氧代类似物，其制备方法及其用途公开了新颖的5-硫杂-1,4-二氮杂双环[4.2 0]辛烷-3,8-二氧代β-内酰胺类似物，其中R 1是氢或卤素; R2是氢，卤素，氨基，PhCH2CONH，PhOCH2CONH，邻苯二甲酰亚氨基，o-MeNHCO-C6H4-CONH，异恶唑基甲酰胺基; R3是氢，烷基，苄基，杂环，例如。 异恶唑，吡唑等，n可以是1或2.它们可以用作制备新型β-内酰胺类似物或用作抗微生物治疗制剂中的活性物质的中间体。

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