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156 条记录 (耗时 0.023 秒)

    Optically active salts of a substituted thiazolidine-4-carboxylate and 3-cyano-hydroxypropyl trimethyl-ammonium, their production and uses
    3.
    发明授权
    Optically active salts of a substituted thiazolidine-4-carboxylate and 3-cyano-hydroxypropyl trimethyl-ammonium, their production and uses 失效
    取代的噻唑烷-4-羧酸酯和3-氰基 - 羟丙基三甲基氨基铵的光学活性物质，其生产和用途

    公开(公告)号：US5191085A

    公开(公告)日：1993-03-02

    申请号：US675623

    申请日：1991-03-27

    申请人： Harald Jakob ,  Klaus Huthmacher ,  Herbert Klenk

    发明人： Harald Jakob ,  Klaus Huthmacher ,  Herbert Klenk

    IPC分类号： C07B53/00 ,  C07C255/26 ,  C07D277/06

    CPC分类号： C07D277/06

    摘要： Optically active salts are disclosed of the formula (I): ##STR1## wherein Ac represents an acyl group, R.sup.1 hydrogen or methyl, R.sup.2 and R.sup.3 identical or different substitutes, preferably methyl. The salts can be obtained from the corresponding optically active carbonic acid and DL-3-cyano-2-hydroxypropyl trimethylammonium hydroxide. The diastereomeric salt pairs are easily split from one another and separated again, so that the process is suited for producing optically active 3-cyano-2-hydroxypropyl trimethylammonium salts.

    摘要翻译： 公开了式（I）的光学活性盐：其中Ac表示酰基，R 1氢或甲基，R 2和R 3相同或不同的取代基，优选甲基。 盐可以从相应的光学活性碳酸和DL-3-氰基-2-羟丙基三甲基铵氢氧化物获得。 非对映体盐对彼此容易分离并再次分离，因此该方法适用于制备光学活性3-氰基-2-羟丙基三甲基铵盐。

    Process for producing L-carnitine from D,L-carnitine nitrile salts
    4.
    发明授权
    Process for producing L-carnitine from D,L-carnitine nitrile salts 失效
    从D，L-CARNITINE NITRILE SALTS生产L-酪氨酸的方法

    公开(公告)号：US5166426A

    公开(公告)日：1992-11-24

    申请号：US858492

    申请日：1992-03-27

    申请人： Harald Jakob ,  Klaus Huthmacher ,  Herbert Klenk

    发明人： Harald Jakob ,  Klaus Huthmacher ,  Herbert Klenk

    IPC分类号： C07B57/00 ,  C07C227/34 ,  C07C229/06

    CPC分类号： C07C227/34

    摘要： Synthesis of L-carnitine by chemical optical resolution of D,L-carnitine nitrile salts, where the D,L-carnitine nitrile salt is reacted with optically active N-acetylproline as the resolving agent in order to form the diastereomer salts after conversion to the hydroxide form, one of the two diastereomer salts is separated by fractional crystallization and the fraction containing mainly L-carnitine nitrile salt is treated with an optically inactive strong acid in order to split off the optically active N-acetylproline and then the resolving agent is separated and the resulting L-carnitine nitrile salt is saponified to L-carnitine. N-acetyl-L-proline is used as the resolving agent and the diastereomer (LL) salt is obtained in crystalline form in a high optical purity by fractional crystallization and the L-carnitine nitrile salt obtained after splitting off and separating N-acetyl-L-proline is used directly for saponification without further crystallization.

    摘要翻译： 通过化学光学拆分D，L-肉碱腈盐合成左旋肉碱，其中D，L-肉毒碱腈与光学活性N-乙酰脯氨酸作为拆分剂反应，以便在转化为 氢氧化物形式，通过分级结晶分离两种非对映异构体盐中的一种，并且用光学惰性的强酸处理主要含有L-肉碱腈盐的级分，以便分离光学活性N-乙酰脯氨酸，然后分离出拆分剂 并将所得的L-肉碱腈盐皂化成L-肉毒碱。 使用N-乙酰基-L-脯氨酸作为拆分剂，通过分级结晶以高光学纯度获得结晶形式的非对映异构体（LL）盐，分解N-乙酰基-L-脯氨酸后得到的L-肉碱腈盐， L-脯氨酸直接用于皂化而不进一步结晶。

    Method of preparing 1,6-di(N.sup.3 -cyano-N.sup.1 -guanidino) hexane
    7.
    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 production of 1,2-dithiolan-3-pentanoic acid (thioctic acid) and 8-hydrocarbylthio-6-oxooctanoic acid
    8.
    发明授权
    Process for the production of 1,2-dithiolan-3-pentanoic acid (thioctic acid) and 8-hydrocarbylthio-6-oxooctanoic acid 失效
    生产1,2-二硫戊环-3-戊酸（硫辛酸）和8-烃基硫代-6-氧代辛酸的方法

    公开(公告)号：US4966732A

    公开(公告)日：1990-10-30

    申请号：US73584

    申请日：1987-07-15

    申请人： Guenes Giray ,  Klaus Huthmacher ,  Axel Kleemann ,  Thomas Lied

    发明人： Guenes Giray ,  Klaus Huthmacher ,  Axel Kleemann ,  Thomas Lied

    IPC分类号： C07C323/52 ,  A61K31/385 ,  A61P1/16 ,  A61P25/00 ,  C07C67/00 ,  C07C313/00 ,  C07C319/06 ,  C07C319/14 ,  C07C319/20 ,  C07C323/22 ,  C07C327/22 ,  C07D339/04

    CPC分类号： C07D339/04 ,  C07C323/00

    摘要： 1,2-Dithiolane-3-pentanoic acid (D,L-thioctic acid) of the formula ##STR1## is prepared by a process comprising (a) reacting a 2-(3-alkylthiopropionyl)-cyclopentanone-1 of the formula ##STR2## where R is a C.sub.1 -C.sub.4 alkyl, phenyl or benzyl in aqueous alkaline solution at a temperature of about 20.degree. C. to about 90.degree. C. to form the corresponding carboxylic acid of formula VI ##STR3## (b) reacting the compound of formula VI with an alkyl mercaptan at a temperature between -20.degree. C. and 0.degree. C. to form the corresponding thioketal of formula VII ##STR4## (c) reacting the compound of formula VII with sodium in liquid ammonia at temperature temperture between -60.degree. C. and -10.degree. C. to form the 6,8-dimercaptooctanic acid of formual VIII ##STR5## (d) reacting the 6,8-dimercaptooctanoic acid of formula VIII in alkaline solution with an iron (III) salt and oxygen to form the 1,2-dithiolane-3-pentanoic acid of formula IX, or in place of steps (a) through (c) reacting an acid of formula XII ##STR6## where R.sub.1 and R.sub.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl or benzyl, with the proviso that both R.sub.1 and R.sub.2 cannot be benzyl, with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the corresponding 6,8-dimercaptooctanoic acid of formula VIII. The compounds of formulae VI, VII, XII are new.

    Process for the production of 1,2-dithiolan-3-pentanoic acid (thioctic acid) and intermediate compounds therefor
    9.
    发明授权
    Process for the production of 1,2-dithiolan-3-pentanoic acid (thioctic acid) and intermediate compounds therefor 失效
    生产1,2-二硫戊环-3-戊酸（硫辛酸）及其中间体化合物的方法

    公开(公告)号：US4705867A

    公开(公告)日：1987-11-10

    申请号：US848212

    申请日：1986-04-04

    申请人： Guenes Giray ,  Klaus Huthmacher ,  Axel Kleemann ,  Thomas Lied

    发明人： Guenes Giray ,  Klaus Huthmacher ,  Axel Kleemann ,  Thomas Lied

    IPC分类号： C07C323/52 ,  A61K31/385 ,  A61P1/16 ,  A61P25/00 ,  C07C67/00 ,  C07C313/00 ,  C07C319/06 ,  C07C319/14 ,  C07C319/20 ,  C07C323/22 ,  C07C327/22 ,  C07D339/04

    CPC分类号： C07D339/04 ,  C07C323/00

    摘要： 1,2-Dithiolane-3-pentanoic acid (D,L-thioctic acid) of the formula ##STR1## is prepared by a process comprising (a) reacting a 2-(3-alkylthiopropionyl)-cyclopentanone-1 of the formula ##STR2## where R is a C.sub.1 -C.sub.4 alkyl, phenyl or benzyl in aqueous alkaline solution at a temperature of about 20.degree. C. to about 90.degree. C. to form the corresponding carboxylic acid of formula VI ##STR3## (b) reacting the compound of formula VI with an alkyl mercaptan at a temperature between -20.degree. C. and 0.degree. C. to form the corresponding thioketal of formula VII ##STR4## (c) reacting the compound of formula VII with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the 6,8-dimercaptooctanoic acid of formula VIII ##STR5## (d) reacting the 6,8-dimercaptooctanoic acid of formula VIII in alkaline solution with an iron (III) salt and oxygen to form the 1,2-dithiolane-3-pentanoic acid of formula IX, or in place of steps (a) through (c) reacting an acid of formula XII ##STR6## where R.sub.1 and R.sub.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl or benzyl, with the proviso that both R.sub.1 and R.sub.2 cannot be benzyl, with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the corresponding 6,8-dimercaptooctanoic acid of formula VIII. The compounds of formulae VI, VII, XII are new.

    摘要翻译： 式（IX）的1,2-二硫戊环-3-戊酸（D，L-硫辛酸）是通过以下方法制备的，该方法包括：（a）使式（I）的2-（3-烷硫基丙酰基） - 环戊酮-1 V，其中R是在约20℃至约90℃的温度下在碱性水溶液中的C 1 -C 4烷基，苯基或苄基，以形成相应的式VI的羧酸 ）使式Ⅵ化合物与烷基硫醇在-20℃至0℃之间的温度下反应，形成相应的式Ⅶ的缩酮醛Ⅶ（c）使式Ⅶ化合物与液体中的钠反应 在-60℃至-10℃的温度下加入氨以形成式VIII的6,8-二巯基辛酸VIII（d）使式VIII的6,8-二巯基辛酸在碱性溶液中与 铁（III）盐和氧气以形成式IX的1,2-二硫戊环-3-戊酸，或代替步骤（a）至（c）使式XI的酸 其中R 1和R 2是氢，C 1 -C 4 - 烷基，苯基或苄基，条件是R 1和R 2不能是苄基，钠在液氨中在-60℃和-60℃之间， 10℃，形成相应的式VIII的6,8-二巯基辛酸。 式VI，VII，XII的化合物是新的。