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

    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

    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。

    Process for the production of 4-amino-6-tert.
butyl-3-mercapto-1,2,4-triazin-5-one
    5.
    发明授权
    Process for the production of 4-amino-6-tert. butyl-3-mercapto-1,2,4-triazin-5-one 失效
    制备4-氨基-6-叔丁氧基羰基的方法。 丁基-3-巯基-1,2,4-三嗪-5-酮

    公开(公告)号:US4326056A

    公开(公告)日:1982-04-20

    申请号:US266147

    申请日:1981-05-22

    IPC分类号: C07D253/06 C07D253/075

    CPC分类号: C07D253/075

    摘要: 4-amino-6-tert.butyl-3-mercapto-1,2,4-triazin-5-one of the formula ##STR1## is produced by reacting pivaloyl cyanide and isobutylene in the presence of acetic acid and sulfuric acid, hydrolyzing the reaction mixture in the presence of water and reacting the trimethyl pyruvic acid formed with thiocarbohydrazide. The triazinone is an important intermediate product in the synthesis of the known herbicide 4-amino-6-tert.butyl-3-methylmercapto-1,2,4-triazin-5-one.

    摘要翻译: 通过在乙酸和硫酸的存在下使新戊酰氰和异丁烯反应制备式“IMAGE”的4-氨基-6-叔丁基-3-巯基-1,2,4-三嗪-5-酮,水解 反应混合物在水存在下反应,并与硫代碳酰肼形成的三甲基丙酮酸反应。 三嗪酮是合成已知除草剂4-氨基-6-叔丁基-3-甲基巯基-1,2,4-三嗪-5-酮的重要中间产物。

    N-Substituted .alpha.-ketocarboxylic acid amides
    9.
    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

    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。

    Process for the production of alpha-ketocarboxylic acid amides and
cycloaliphatic products
    10.
    发明授权
    Process for the production of alpha-ketocarboxylic acid amides and cycloaliphatic products 失效
    制备α-酮羧酸酰胺和脂环族产物的方法

    公开(公告)号:US4161491A

    公开(公告)日:1979-07-17

    申请号:US802903

    申请日:1977-06-02

    CPC分类号: C07C231/06

    摘要: There are prepared .alpha.-ketocarboxylic acid amides of the formula ##STR1## where R is hydrogen, R.sub.1 and R.sub.2 are the same or different, R.sub.1 is alkyl of 1 to 18 carbon atoms or haloalkyl, preferably chloroalkyl, of 1 to 18 carbon atoms, and R.sub.2 is hydrogen, alkyl of 1 to 18 carbon atoms or haloalkyl, preferably chloroalkyl, of 1 to 18 carbon atoms or ##STR2## together is a cycloalkyl group of 3 to 8 carbon atoms which can be substituted by one or more 1 to 5 carbon atom alkyl groups or by one or more halogen atoms, preferably chlorine atoms, with the proviso that when ##STR3## form a cycloalkyl group then R can also be alkyl of 1 to 5 carbon atoms. The process comprises saponifying an acyl cyanide of the formula ##STR4## in which R, R.sub.1 and R.sub.2 are as defined above in an organic solvent or mixture of such solvents which is liquid and inert under the reaction conditions, first with gaseous hydrogen chloride and then treating with water at a temperature of about -70.degree. C. to about +70.degree. C. and then isolating the .alpha.-ketocarboxylic acid amide in conventional manner. Several of the cyclic .alpha.-ketocarboxylic acid amides are new compounds.

    摘要翻译: 制备式(I)的α-酮羧酸酰胺,其中R是氢,R 1和R 2相同或不同,R 1是1至18个碳原子的烷基或卤代烷基,优选氯代烷基,其为1至18 碳原子,R 2是氢,1至18个碳原子的烷基或具有1至18个碳原子的卤代烷基,优选氯代烷基,或者“IMAGE”是3-8个碳原子的环烷基,其可以被一个或多个 1至5个碳原子的烷基或一个或多个卤素原子,优选氯原子,条件是当形成环烷基时,则R也可以是1至5个碳原子的烷基。 该方法包括在其中R 1,R 2和R 2如上所定义的式(Ⅶ)的酰基氰在有机溶剂或这种在反应条件下为液体和惰性的溶剂的混合物中,首先用气态氢 然后在约-70℃至约+70℃的温度下用水处理,然后以常规方式分离α-酮羧酸酰胺。 几种环状α-酮羧酸酰胺是新的化合物。