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    Dithienylpiperidines, pharmaceutical compositions thereof, and method of use thereof
    52.
    发明授权
    Dithienylpiperidines, pharmaceutical compositions thereof, and method of use thereof 失效
    二噻吩基哌啶，其药物组合物及其使用方法

    公开(公告)号：US4283405A

    公开(公告)日：1981-08-11

    申请号：US112099

    申请日：1980-01-14

    申请人： Jurgen Engel ,  Axel Kleemann ,  Fritz Stroman ,  Klaus Thiemer

    发明人： Jurgen Engel ,  Axel Kleemann ,  Fritz Stroman ,  Klaus Thiemer

    IPC分类号： C07D409/14 ,  A61K20060101 ,  A61K31/38 ,  A61K31/4433 ,  A61K31/445 ,  A61P7/06 ,  A61P9/02 ,  A61P25/04 ,  C07D20060101

    CPC分类号： A61K31/38 ,  A61K31/4433 ,  A61K31/445 ,  C07D409/14

    摘要： There are prepared compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together represent a second bond between the carbon atom carrying R.sub.1 and R.sub.2, R.sub.1 also can be a hydroxy group, R.sub.3 is hydrogen, a C.sub.3 -C.sub.8 cycloalkyl group or a C.sub.1 -C.sub.20 alkyl group, which optionally can also contain one or two hydroxy groups and the groups R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen, C.sub.1 -C.sub.6 -alkyl groups or halogen atoms, their N-oxide, their quaternary salts and their acid addition salts. There are also described processes for their production. The compounds possess especially an antischemic and blood pressure increasing activity.

    摘要翻译： 制备式Ⅰ的化合物，其中R1和R2是氢或一起代表携带R1和R2的碳原子之间的第二个键，R1也可以是羟基，R3是氢，C3-C8环烷基 或C 1 -C 20烷基，其任选地还可以含有一个或两个羟基，并且基团R 4，R 5，R 6和R 7相同或不同，并且是氢，C 1 -C 6 - 烷基或卤素原子， 氧化物，它们的季盐和它们的酸加成盐。 还描述了其生产方法。 这些化合物特别具有抗缺血和增压活性。

    N-Substituted .alpha.-ketocarboxylic acid amides
    53.
    发明授权
    N-Substituted .alpha.-ketocarboxylic acid amides 失效
    N-取代的α-酮羧酸酰胺

    公开(公告)号：US4228082A

    公开(公告)日：1980-10-14

    申请号：US56084

    申请日：1979-07-09

    申请人： Axel Kleemann ,  Herbert Klenk ,  Heribert Offermanns ,  Paul Scherberich ,  Werner Schwarze

    发明人： Axel Kleemann ,  Herbert Klenk ,  Heribert Offermanns ,  Paul Scherberich ,  Werner Schwarze

    IPC分类号： A01N25/00 ,  A01P3/00 ,  A01P13/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/06 ,  C07C231/08 ,  C07C235/72 ,  C07D307/54 ,  C07C103/737 ,  C07C103/76

    CPC分类号： C07D307/54

    摘要： Compounds are prepared of the formula ##STR1## where R' is a t-alkyl group having 4 to 18 carbon atoms, preferably t-butyl, t-amyl or t-octyl and R is a straight or branched chain alkyl group with 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms or an alkyl group substituted with one or more phenyl group or a halogen atom, particularly a chlorine atom, or a cycloalkyl group with 3 to 8 carbon atoms, particularly cyclopropyl, which can be substituted by one or more 1 to 3 carbon atom alkyl groups or one or more halogen atoms, preferably chlorine, or phenyl or naphthyl or a five membered heterocyclic group or such phenyl, naphthyl or heterocyclic group substituted by halogen atoms, nitro groups, alkyl or alkoxy with 1 to 5 carbon atoms by condensing in acid medium an acyl cyanide of the formulaR--CO--CN (II)where R is as defined above with either(a) a tertiary alcohol of the formulaHO--R' (III) in which R' is as defined above, or preferably(b) an alkene of the formula ##STR2## where R.sub.1 and R.sub.2 are the same or different and are hydrogen or an alkyl group and wherein R.sub.3 and R.sub.4 are the same or different and wherein the alkyl groups in each case can be 1 to 15 carbon atoms. Some of the compounds are new. They are useful as intermediates for synthesizing herbicides and can be used directly as fungicides.

    摘要翻译： 化合物由式（I）制备，其中R'是具有4至18个碳原子的叔烷基，优选叔丁基，叔戊基或叔辛基，R是直链或支链烷基 具有1至18个碳原子，优选1至10个碳原子的烷基或被一个或多个苯基或卤素原子，特别是氯原子或具有3至8个碳原子的环烷基特别是环丙基取代的烷基，其可以 被一个或多个1至3个碳原子的烷基或一个或多个卤素原子，优选氯，或苯基或萘基或五元杂环基或被卤素原子取代的苯基，萘基或杂环基，硝基，烷基 或具有1至5个碳原子的烷氧基，通过在酸性介质中缩合式R-CO-CN（II）的酰基氰，其中R如上定义，与（a）式HO-R'（III ），其中R'如上所定义，或优选（b）下式的烯烃（I） V）其中R 1和R 2相同或不同并且是氢或烷基，并且其中R 3和R 4相同或不同，并且其中每种情况下的烷基可以是1至15个碳原子。 一些化合物是新的。 它们可用作合成除草剂的中间体，可直接用作杀真菌剂。

    Method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane
    58.
    发明授权
    Method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane 失效
    制备1,6-二（N 3 - 氰基-N 1胍基）己烷的方法

    公开(公告)号：US5041655A

    公开(公告)日：1991-08-20

    申请号：US241116

    申请日：1988-09-06

    申请人： Klaus Huthmacher ,  Axel Kleemann ,  Horst Bethge ,  Rolf Braun

    发明人： Klaus Huthmacher ,  Axel Kleemann ,  Horst Bethge ,  Rolf Braun

    IPC分类号： C07C67/00 ,  C07C239/00 ,  C07C277/08 ,  C07C279/28

    CPC分类号： C07C279/28

    摘要： An improved method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane from alkali dicyanamide and a hexamethylene diammonium salt in alcoholic solution or suspension. The reaction is carried out in the presence of a limited amount of water and of a catalytic amount of a base, preferably a tertiary amine. The pH of the reaction mixture at the start of the reaction is 8 to 10. After the reaction is over, the reaction mixture is compounded with water at a temperature above 80.degree. C. and the coarse product which crystallizes out is separated from the liquid phase.Preferably, sodium dicyanamide and hexamethylene diamine dihydrochloride, preferably formed in situ from aqueous 1,6-diaminohexane and aqueous hydrochloric acid, are reacted at pH 9-9.5 in n-butanol in the presence of 0.1 to 20% by wt. water in relation to the solvent including water.1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane is obtained in a high yield (85-86%) and with great purity (95-97%) and with a considerably improved space-time yield.

    摘要翻译： 一种在醇溶液或悬浮液中由碱二氰胺和六亚甲基二铵盐制备1,6-二（N 3 - 氰基-N 1胍基）己烷的改进方法。 反应在有限量的水和催化量的碱，优选叔胺的存在下进行。 反应开始时反应混合物的pH值为8〜10。反应结束后，将反应混合物在高于80℃的温度下与水混合，将结晶出来的粗产物与液体分离 相。 优选地，优选在1,6-二氨基己烷水溶液和盐酸水溶液中原位形成的二氰胺钠和六亚甲基二胺盐酸盐在pH为9-9.5的正丁醇中，在0.1-20重量％的存在下反应。 相对于包括水在内的溶剂的水。 以高产率（85-86％）和高纯度（95-97％）获得1,6-二（N 3 - 氰基-N 1胍基）己烷，并具有显着提高的时空产率。

    Process for the isolation of L-amino acids
    59.
    发明授权
    Process for the isolation of L-amino acids 失效
    L-氨基酸分离方法

    公开(公告)号：US4827029A

    公开(公告)日：1989-05-02

    申请号：US146637

    申请日：1988-01-21

    申请人： Axel Kleemann ,  Kurt Klostermann ,  Wolfgang Leuchtenberger ,  Rudi E. Moerck ,  Michael Karrenbauer

    发明人： Axel Kleemann ,  Kurt Klostermann ,  Wolfgang Leuchtenberger ,  Rudi E. Moerck ,  Michael Karrenbauer

    IPC分类号： B01J39/26 ,  C07C227/34 ,  C07C227/40 ,  C07C229/02 ,  C07C319/28 ,  C07C323/58 ,  C12P13/04 ,  C07C99/12

    CPC分类号： C12P13/04

    摘要： L-amino acids present in cleavage solutions obtained in the acylase-catalyzed cleavage of N-acetyl-D,L-amino acids are isolated by use of a strongly acidic ion exchanger in H+ form. First, the mother liquor from a previous treatment cycle is fed to the ion exchanger, and then the cleavage solution and finally the wash water and the discharge from the ion exchanger which is pH-controlled is analyzed into an "effluent water fraction", an "N-acetyl-D-amino acid fraction" and an "L-amino acid fraction". The last fraction is adjusted by addition of fresh cleavage solution to a pH of between 4.0 and 6.0, and from the mixture which is thus obtained the L-amino acid is isolated by crystallization. The mother liquor which is obtained is recycled back into a subsequent treatment cycle.

    摘要翻译： 通过使用H +形式的强酸性离子交换剂分离存在于酰基转移酶催化的N-乙酰基-D，L-氨基酸切割中获得的切割溶液中的L-氨基酸。 首先，将来自先前处理循环的母液进料到离子交换器中，然后将分离溶液，最后洗涤水和从pH离子交换器排出的pH值控制分析为“流出水分数”， “N-乙酰基-D-氨基酸级分”和“L-氨基酸级分”。 通过将新鲜裂解溶液加入至4.0至6.0的pH来调节最后的级分，并且由此得到的混合物通过结晶分离L-氨基酸。 将获得的母液循环回到随后的处理循环中。