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    2-bromo-and derivatives of 3-bromo-and 3,3-dibromo-4-oxo-azetidines, processes for the preparation thereof and use thereof
    301.
    发明授权
    2-bromo-and derivatives of 3-bromo-and 3,3-dibromo-4-oxo-azetidines, processes for the preparation thereof and use thereof 失效
    3-溴 - 和3,3-二溴-4-氧代 - 氮杂环丁烷的2-溴衍生物，其制备方法及其用途

    公开(公告)号：US5847119A

    公开(公告)日：1998-12-08

    申请号：US624919

    申请日：1996-03-27

    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: 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 are provided. The azetidines of the present invention have the formula I ##STR1## wherein R.sup.1 is hydrogen or bromine, R.sup.2 is hydrogen or bromine, wherein at least one of R.sup.1 or R.sup.2 is bromine, R.sup.3 is hydrogen; Me.sub.2 --C.dbd.C--COOR.sup.4 wherein R.sup.4 is hydrogen, methyl, benzyl or some other carboxy-protective group, and X is bromine or nitroxy group (--ONO.sub.2). 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, antitumour or antagonistic action.

    Abstract translation: 提供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。 本发明的氮杂环丁烷具有式I其中R 1是氢或溴，R 2是氢或溴，其中R 1或R 2中的至少一个是溴，R 3是氢; Me2-C = C-COOR4，其中R4是氢，甲基，苄基或一些其它羧基保护基，X是溴或硝基氧基（-ONO 2）。 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的DBN盐或分离的亚磺酸用亚硫酰氯处理，通过蒸发除去亚硫酰氯后，将所得残余物通过硅胶柱， 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，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菌，抑制，抗肿瘤或拮抗作用的制剂中的组分的有用中间体。

    Preparation of N-substituted lactams
    302.
    发明授权
    Preparation of N-substituted lactams 失效
    N-取代的内酰胺的制备

    公开(公告)号：US5276165A

    公开(公告)日：1994-01-04

    申请号：US982300

    申请日：1992-11-25

    Applicant: Hans-Juergen Weyer ,  Rolf Fischer

    Inventor： Hans-Juergen Weyer ,  Rolf Fischer

    IPC: B01J21/04 ,  B01J23/28 ,  B01J23/34 ,  B01J23/72 ,  B01J23/75 ,  C07B61/00 ,  C07D201/02 ,  C07D201/08 ,  C07D207/26 ,  C07D207/267 ,  C07D209/46 ,  C07D209/64 ,  C07D223/10 ,  C07D225/02 ,  C07D207/12 ,  C07D221/06

    CPC classification number: C07D201/02 ,  C07D201/08 ,  C07D207/267

    Abstract: A process for the preparation of N-substituted lactams of the formula I ##STR1## where Z is C.sub.2 - to C.sub.10 -alkylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andR.sup.1 is C.sub.1 - to C.sub.20 -alkyl, C.sub.6 - to C.sub.10 -aryl or C.sub.7 - to C.sub.12 -aralkyl,by hydrogenating a compound of the formula II ##STR2## where W is C.sub.2 - to C.sub.10 -alkylene, C.sub.2 - to C.sub.10 -alkenylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andX and Y together form an oxa or imido bridge of the formula ##STR3## or alternatively are identical or different and are hydroxyl, C.sub.1 - to C.sub.20 -alkoxy, C.sub.6 - to C.sub.10 -aryloxy or C.sub.7 - to C.sub.12 -aralkoxy, and, if X and Y are different, Y, in addition to the abovementioned meanings, may also be hydrogen,at superatmospheric pressure and at elevated temperature in the presence of a catalyst and in the presence of an amine, which comprises using a secondary and/or tertiary amine of the formula IIINH.sub.n R.sub.3-n .sup.1where R.sup.1 is as defined above and n is 0 or 1, or a mixture of a secondary and/or teritary amine of this type with a primary amine of the formula IVR.sup.1 --NH.sub.2 (IV)as the starting material, and carrying out the reaction with addition of water and/or ammonia.

    Abstract translation: 制备式I的N-取代的内酰胺的方法（I）其中Z为C 2至C 10亚烷基，C 7至C 12 - 亚芳基，亚苯基或亚萘基，R 1为C 1 -C 20烷基 C 6 -C 10 - 芳基或C 7 - 至C 12 - 芳烷基，其中W是C 2 - 至C 10 - 亚烷基，C 2至C 10亚烯基，C 7 - 至C 12 - 亚烷基， - 亚烷基，亚苯基或亚萘基，X和Y一起形成下式的氧杂或亚氨基桥，或者可选地相同或不同，为羟基，C 1至C 20 - 烷氧基，C 6至C 10 - 芳氧基或C 7 - 对于C 12 - 芳烷氧基，并且如果X和Y不同，除了上述含义之外，Y还可以是氢，在超大气压和升高的温度下，在催化剂的存在下和在胺的存在下， 包括使用式III NH n R 3-n 1的仲和/或叔胺，其中R 1如上定义并且n为0或1，或者该仲胺和/或叔胺的混合物 以式ⅣR-NH2（Ⅳ）的伯胺为起始原料，并加入水和/或氨进行反应。

    Process for producing cyanovaleric esters and caprolactam
    303.
    发明授权
    Process for producing cyanovaleric esters and caprolactam 失效
    制备氰戊酸酯和己内酰胺的方法

    公开(公告)号：US4470928A

    公开(公告)日：1984-09-11

    申请号：US420883

    申请日：1982-09-21

    Applicant: Kohji Kimura ,  Toshiro Isoya

    Inventor： Kohji Kimura ,  Toshiro Isoya

    IPC: C07D201/02 ,  C07D201/08 ,  C07D223/08 ,  C07D223/10 ,  C07C120/00 ,  C07C121/16 ,  C07C121/407

    CPC classification number: C07C255/00 ,  C07D201/08 ,  Y02P20/52

    Abstract: Caprolactam can be produced with an economical advantage without formation of by-products in a high yield by subjecting adipic acid and adiponitrile to interchange reaction at an elevated temperature, adding an alcohol directly to the interchange reaction mixture without isolating the resulting cyanovaleric acid to esterify the cyanovaleric acid with said alcohol into a cyanovaleric ester, reducing the cyanovaleric ester with a catalyst into an aminocaproic ester, heating the aminocaproic ester in a polyhydric alcohol having a higher boiling point than that of caprolactam to convert the ester into caprolactam, isolating the caprolactam by distillation and recycling the liquid distillation residue to the system for heating said polyhydric alcohol and said aminocaproic ester.

    Abstract translation: 可以生产具有经济优势的己内酰胺，而不会通过使己二酸和己二腈在升高的温度下进行交换反应而以高产率形成副产物，直接向交换反应混合物中加入醇，而不分离得到的氰基戊酸酯化 将氰基戊酸与所述醇反应成氰基戊酸酯，用催化剂将氰基戊酸酯还原成氨基己酸酯，加热沸点高于己内酰胺的多元醇中的氨基己酸酯将酯转化为己内酰胺，将己内酰胺转化为己内酰胺 蒸馏并将液体蒸馏残余物再循环到用于加热所述多元醇和所述氨基己酸酯的体系中。

    Purification of caprolactam
    304.
    发明授权
    Purification of caprolactam 失效
    己内酰胺的纯化

    公开(公告)号：US4301073A

    公开(公告)日：1981-11-17

    申请号：US160308

    申请日：1980-06-17

    Applicant: Hugo Fuchs ,  Otto-Alfred Grosskinsky ,  Elmar Frommer ,  Klaus Kartte

    Inventor： Hugo Fuchs ,  Otto-Alfred Grosskinsky ,  Elmar Frommer ,  Klaus Kartte

    IPC: C07D201/02 ,  C07D201/16 ,  C07D223/10

    CPC classification number: C07D201/16

    Abstract: A process for purifying caprolactam, which has been obtained by a Beckmann rearrangement, by extracting crude caprolactam with solvents, distilling the extract in the presence of alkali, and isolating pure caprolactam, wherein, in a first stage, caprolactam is distilled from the alkaline distillation residue at a bottom temperature of 130.degree.-160.degree. C., and is recycled to the distillation stage, the residue thus obtained is distilled, in a second stage, at a bottom temperature of 140.degree.-180.degree. C., and the distillate is treated with strongly acidic agents in a third stage and is then recycled to the extraction stage.

    Abstract translation: 一种通过贝克曼重排获得的己内酰胺的纯化方法，用溶剂萃取粗己内酰胺，在碱存在下蒸馏提取物，并分离纯己内酰胺，其中在第一阶段中，从碱性蒸馏中蒸馏己内酰胺 残余物在130℃-160℃的底部温度下再循环至蒸馏阶段，所得残余物在第二阶段在140-180℃的底部温度下蒸馏，馏出物 在第三阶段用强酸性剂处理，然后再循环至萃取阶段。

    Conversion of 2-dialkylamino-3H-azepines into epsilon caprolactams
    307.
    发明授权
    Conversion of 2-dialkylamino-3H-azepines into epsilon caprolactams 失效
    2-二烷基氨基-3H-氮杂转化为ε己内酰胺

    公开(公告)号：US4110323A

    公开(公告)日：1978-08-29

    申请号：US741838

    申请日：1976-11-15

    Applicant: Sylvain A. R. Dewaele

    Inventor： Sylvain A. R. Dewaele

    IPC: C07D201/02 ,  C07D223/12

    CPC classification number: C07D201/02 ,  C07D223/12

    Abstract: This invention relates to a process of catalytically converting nitrobenzene to 2-amino-3H-azepines by the reaction of the nitrobenzene with trisaminophosphine and an amine of the formula HNR'.sub.2, where R' is lower alkyl containing 1 to 6 carbon atoms.In addition, this invention concerns the catalytic hydrogenation of 2-amino-3H-azepine to epsilon caprolactam.

    Abstract translation: 本发明涉及通过硝基苯与三氨基膦的反应和式HNR'2的胺反应将硝基苯催化转化为2-氨基-3H-吖庚因的方法，其中R'是含有1至6个碳原子的低级烷基。

    Azetidine derivatives
    308.
    发明授权
    Azetidine derivatives 失效
    氮杂环丁烷衍生物

    公开(公告)号：US4007202A

    公开(公告)日：1977-02-08

    申请号：US547948

    申请日：1975-02-07

    Applicant: Jan Verweij ,  Hong Sheng Tan

    Inventor： Jan Verweij ,  Hong Sheng Tan

    IPC: C07D205/08 ,  A61K31/545 ,  C07D201/02 ,  C07D205/095 ,  C07D207/46 ,  C07D209/48 ,  C07D401/12 ,  C07D403/12 ,  C07D501/08 ,  C07D501/10 ,  C07D501/30 ,  C07D501/60 ,  C07D207/12

    CPC classification number: C07D209/48 ,  C07D207/46

    Abstract: Novel azetidine derivatives of the formula ##STR1## wherein R.sub.1 is an acylamido group, R.sub.2 is selected from the group consisting of ##STR2## wherein R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, lower alkyl and lower alkenyl, n is 2 or 3 and -- in the case when formula IIB is a phenyl - this group may carry one to four substituents selected from the group consisting of halogen, lower alkyl, lower alkenyl and phenyl, and R.sub.3 is lower alkyl optionally substituted with 1 or 2 phenyls which phenyl groups may be substituted with nitro and the dotted lines of formula IIB indicate the optional presence of double bonds and a process for their preparation and process for the preparation of cephalosporanic acid derivatives using the azetidines of formula I as intermediates.

    Abstract translation: 新颖的式Ⅰa的氮杂环丁烷衍生物，其中R 1是酰氨基，R 2选自其中R 4，R 5和R 6各自独立地选自下列的组合：IIA IIB IIC IID 由氢，低级烷基和低级烯基组成的组，n为2或3， - 在式IIB为苯基的情况下，该基团可以携带一至四个选自以下的取代基：卤素，低级烷基，低级 烯基和苯基，R3是任选被1或2个苯基取代的低级烷基，该苯基可以被硝基取代，式IIB的虚线表示双键的任选存在，以及它们的制备方法和制备方法 使用式I的氮杂环丁烷的头孢烷酸衍生物作为中间体。

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