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    Process for preparation of penam derivatives
    5.
    发明申请
    Process for preparation of penam derivatives 审中-公开
    Penam衍生物的制备方法

    公开(公告)号：US20060173177A1

    公开(公告)日：2006-08-03

    申请号：US11046080

    申请日：2005-01-28

    申请人： Csaba Gego ,  Imre Fejes ,  Imre Kovacs ,  Ferenc Lukacs ,  Geza Schneider

    发明人： Csaba Gego ,  Imre Fejes ,  Imre Kovacs ,  Ferenc Lukacs ,  Geza Schneider

    IPC分类号： C07D499/12

    CPC分类号： C07D499/00

    摘要： The invention relates to novel processes for preparing penam derivatives, such as Tazobactam and derivatives thereof. The processes according to the invention encompass procedures for the protection and deprotection of the carboxylic group as well as for the oxidation of the sulfur moiety of penam derivatives. Additionally, the present invention relates to new intermediates for the production of penam derivatives, allowing the desired penam-derivatives to be formulated with high purity and in good yields.

    摘要翻译： 本发明涉及制备penam衍生物的新方法，如他唑巴坦及其衍生物。 根据本发明的方法包括羧基的保护和脱保护以及对于penam衍生物的硫部分的氧化的方法。 此外，本发明涉及用于生产penam衍生物的新中间体，使得所需的penam衍生物以高纯度和良好的产率配制。

    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives
    6.
    发明授权
    Anorexigenic 4-[(3,4-dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives 失效
    厌氧性4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑烷酮衍生物

    公开(公告)号：US4308278A

    公开(公告)日：1981-12-29

    申请号：US90450

    申请日：1979-11-01

    申请人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    发明人： Geza Schneider ,  Ferenc Andrasi ,  Pal Berzsenyi ,  Arpad Lazar ,  Sandor Elek ,  Istvan Elekes ,  Istvan Polgari

    IPC分类号： A61K31/415 ,  A61K31/4166 ,  A61P1/00 ,  A61P3/04 ,  C07C45/71 ,  C07D233/32 ,  C07D233/34 ,  C07D233/38 ,  C07D233/78

    CPC分类号： C07C255/00 ,  C07C45/71 ,  C07D233/32 ,  C07D233/38 ,  C07D233/78 ,  Y10S514/91

    摘要： 4-[(3,4-Dialkoxyphenyl)alkyl]-2-imidazolidinone derivatives having the formula I ##STR1## wherein R.sup.1 stands for a cycloalkyl group containing from 3 to 6 carbon atoms or benzyl group;R.sup.2 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.3 stands for hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms;R.sup.4 stands for hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms or an alkoxycarbonyl group containing from 1 to 4 carbon atoms; andR.sup.5 stands for hydrogen atom or an alkoxycarbonyl group containing from 1 to 4 carbon atoms,are prepared by(a) reducing a hydantoin derivative having the general formula II, wherein R.sup.1 and R.sup.2 are as defined above, with lithium aluminum hydride in a neutral organic solvent, or(b) hydrogenating catalytically an 1,3-dihydro-2H-imidazol-2-one derivative having the general formula III, wherein R.sup.1 and R.sup.3 are as defined above, while the meaning of R.sup.4 is hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, or(c) reacting a carbamate derivative having the general formula IV, wherein R.sup.1 is as defined above, while R.sup.6 stands for an alkyl group containing from 1 to 4 carbon atoms, with an organic or inorganic base.The compounds having the formula I possess valuable therapeutical properties, mainly anorexigenic activity.

    摘要翻译： 4 - [（3,4-二烷氧基苯基）烷基] -2-咪唑啉酮衍生物，其具有式I其中R1代表含有3至6个碳原子的环烷基或苄基; R2代表氢原子或含有1至4个碳原子的烷基; R3代表氢原子或含有1至4个碳原子的烷基; R4表示氢原子或含有1至4个碳原子的烷基或含有1至4个碳原子的烷氧基羰基; 并且R5代表氢原子或含有1至4个碳原子的烷氧基羰基，是通过以下步骤制备的：（a）将具有通式II的乙内酰脲衍生物（其中R 1和R 2如上定义）与中性的氢化铝锂 有机溶剂，或（b）催化氢化具有通式III的1,3-二氢-2H-咪唑-2-酮衍生物，其中R 1和R 3如上所定义，而R 4的含义是氢原子或烷基 含有1至4个碳原子的基团，或（c）使具有通式IV的氨基甲酸酯衍生物与其中R 1如上定义，而R6代表含有1至4个碳原子的烷基，与有机或无机 基础。 具有式I的化合物具有有价值的治疗性质，主要是厌食症活性。