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    Process for the production of acyl cyanides (B)
    24.
    发明授权
    Process for the production of acyl cyanides (B) 失效
    酰基氰生产工艺（二）

    公开(公告)号：US4108875A

    公开(公告)日：1978-08-22

    申请号：US802942

    申请日：1977-06-02

    Applicant: Herbert Klenk ,  Heribert Offermanns ,  Werner Schwarze

    Inventor： Herbert Klenk ,  Heribert Offermanns ,  Werner Schwarze

    IPC: C07C253/14 ,  B01J23/00 ,  B01J27/00 ,  C07B61/00 ,  C07C67/00 ,  C07C253/00 ,  C07C255/17 ,  C07C255/18 ,  C07C255/31 ,  C07C255/40 ,  C07C255/45 ,  C07C255/53 ,  C07C255/56 ,  C07D307/06 ,  C07D307/54 ,  C07D307/56 ,  C07D333/04 ,  C07D333/22 ,  C07D333/24 ,  C07D307/36 ,  C07C57/00 ,  C07C63/06

    CPC classification number: C07C255/00 ,  C07C253/14 ,  C07D307/54 ,  C07D333/24

    Abstract: There are prepared acyl cyanides of the formula ##STR1## where R is a straight or branched chain alkyl group having 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms, and which also can be substituted by one or more phenyl groups or halogen atoms, preferably chlorine, or R is preferably a cycloalkyl group having 3 to 8 carbon atoms, preferably cyclopropyl, which can have one or more 1 to 3 carbon atom alkyl or halogen, preferably chlorine, substituents wherein in all of the above set forth substitutions the halogen atoms and the phenyl groups are not on the carbon atom adjacent to the carbonyl group or R is a substituted phenyl group, a naphthyl group, a substituted naphthyl group or a five membered heterocyclic group, e.g., furyl, thienyl or alkyl substituted thienyl, wherein the substituents on the phenyl or naphthyl are halogen atoms, nitro groups or alkyl or alkoxy groups having 1 to 5 carbon atoms. The process comprises reacting an acyl halide of the formulaR--CO--Hal (II)in which R is as defined above and Hal is a chlorine or bromine atom, with a mixture consisting of about 0.1 to 5 equivalents of the alkali metal cyanide and about 0.05 to 2 equivalents of the copper (I) salt at a temperature of about 50.degree. to 180.degree. C in the presence of a carboxylic acid nitrile inert under the reaction conditions employed. Certain of the compounds are novel per se.

    Abstract translation: 制备式（I）的酰基氰化物，其中R是具有1至18个碳原子，优选1至10个碳原子的直链或支链烷基，并且也可被一个或多个苯基取代 或卤素原子，优选氯，或R优选为具有3至8个碳原子的环烷基，优选环丙基，其可以具有一个或多个1至3个碳原子的烷基或卤素，优选氯，取代基，其中在上述所有 卤素原子和苯基不在与羰基相邻的碳原子上，或者R是取代的苯基，萘基，取代的萘基或五元杂环基，例如呋喃基，噻吩基或烷基 取代的噻吩基，其中苯基或萘基上的取代基是卤素原子，硝基或具有1-5个碳原子的烷基或烷氧基。 该方法包括使式R-CO-Hal（II）的酰卤，其中R如上定义，Hal是氯或溴原子，与由约0.1至5当量的碱金属氰化物和 在约50至180℃的温度下，在所用反应条件下在惰性的羧酸腈存在下，约0.05-2当量的铜（I）盐。 某些化合物本身是新颖的。

    Sulfur containing trialkoxybenzoylamino carboxylic acids
    25.
    发明授权
    Sulfur containing trialkoxybenzoylamino carboxylic acids 失效
    含有三烷氧基苯甲酰氨基羧酸的硫

    公开(公告)号：US4055653A

    公开(公告)日：1977-10-25

    申请号：US687504

    申请日：1976-05-18

    Applicant: Heribert Offermanns ,  Klaus Posselt

    Inventor： Heribert Offermanns ,  Klaus Posselt

    IPC: C07D333/36 ,  A61K31/24 ,  A61K31/195 ,  A61K31/38

    CPC classification number: C07D333/36

    Abstract: Compounds are prepared of the formula: ##STR1## wherein A is a straight or branched chain alkylene or alkylidene radical having 2 to 5 carbon atoms and which is substituted by an alkylthio group having 1 to 4 carbon atoms, a carboxymethyl thio group, a carboxyethyl thio group, an alkylsulfonyl group having 1 to 4 carbon atoms, a mercapto group, or the substituent on A together with --COR.sub.4 forms a 4 to 7 membered thiolactone ring, or A is substituted by an acylmercapto group wherein the acyl is benzoyl, a benzoyl radical substituted with one, two or three alkoxy groups with 1 to 6 carbon atoms, an alkanoyl radical of 1 to 6 carbon atoms, an alkenoyl radical of 3 to 6 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 are the same or different and are alkyl groups of 1 to 5 carbon atoms and one of R.sub.1, R.sub.2 and R.sub.3 also can be hydrogen or the acyl radical of an alkanoic acid of 2 to 4 carbon atoms and R.sub.4 is a hydroxy group or an alkoxy group with 1 to 5 carbon atoms and their pharmacologically acceptable salts. The compounds are pharmacodynamically active and are suited for prophylaxis and treatment of heart illnesses such as cardiac ischemia, cardiac infarct, heart rhythm and circulatory disturbances.

    Abstract translation: 化合物由下式制备：其中A是具有2至5个碳原子并且被具有1至4个碳原子的烷硫基取代的直链或支链亚烷基或亚烷基，羧甲基硫代基， 羧基乙基硫基，碳原子数为1〜4的烷基磺酰基，巯基或者与-COR 4一起形成的取代基形成4〜7元的硫醇内酯环，或者A被酰基巯基取代，其中酰基是苯甲酰基， 被1〜2个碳原子的1〜2个碳原子的烷氧基取代的苯甲酰基，1〜6个碳原子的烷酰基，3〜6个碳原子的烯酰基，R1，R2和R3相同或不同， 是1〜5个碳原子的烷基，R1，R2和R3中的一个也可以是氢或2〜4个碳原子的链烷酸的酰基，R4是羟基或具有1〜5个碳原子的烷氧基 原子及其药理学上可接受的盐。 该化合物具有药效学活性，适用于预防和治疗心脏病，如心脏缺血，心肌梗塞，心律和循环障碍。

    Process of preparing penicillamine
    26.
    发明授权
    Process of preparing penicillamine 失效
    制备青霉胺的方法

    公开(公告)号：US4045479A

    公开(公告)日：1977-08-30

    申请号：US598995

    申请日：1975-07-25

    Applicant: Friedrich Asinger ,  Heribert Offermanns ,  Karl-Heinz Gulzek

    Inventor： Friedrich Asinger ,  Heribert Offermanns ,  Karl-Heinz Gulzek

    IPC: C07D277/06 ,  C07D277/10 ,  C07C99/00

    CPC classification number: C07D277/06 ,  C07D277/10

    Abstract: Penicillamine or a homolog thereof is made by reacting an aldehyde branched at the .alpha.-carbon atom, sulfur and ammonia to form a thiazoline- .DELTA..sup.3 ; converting the latter compound by reaction with anhydrous hydrogen cyanide into the corresponding thiazolidine-4-carbonitrile; hydrolyzing the nitrile with an aqueous concentrated hydrochloric acid containing at least 30% by weight of hydrogen chloride at a temperature between 40.degree. and 70.degree. C to form the hydrochloric salt of the thiazolidine-4-acid amide and then, at a higher temperature continuing the hydrolysis to form the salt of the thiazolidine-4-carboxylic acid together with the ammonium salt. The ammonium salt is then separated from the mixture and the carboxylic acid hydrochloride is hydrolytically decomposed whereby the penicillamine is obtained.

    Abstract translation: 青霉胺或其同系物通过使在α-碳原子上分支的醛，硫和氨反应形成噻唑啉-TATA 3而制备; 通过与无水氰化氢反应将后一种化合物转化成相应的噻唑烷-4-腈; 在40℃〜70℃的温度下，用含有至少30重量％氯化氢的浓盐酸水解腈，形成噻唑烷-4-酸酰胺的盐酸盐，然后在更高的温度下继续 水解形成噻唑烷-4-羧酸的盐与铵盐一起。 然后将铵盐与混合物分离，并将羧酸盐酸盐水解分解，从而得到青霉胺。

    2-Benzoyl-3-amino-pyridines
    27.
    发明授权
    2-Benzoyl-3-amino-pyridines 失效
    2-苯甲酰基-3-氨基 - 吡啶

    公开(公告)号：US4012397A

    公开(公告)日：1977-03-15

    申请号：US661817

    申请日：1976-02-26

    Applicant: Walter von Bebenburg ,  Heribert Offermanns

    Inventor： Walter von Bebenburg ,  Heribert Offermanns

    IPC: C07D213/57 ,  C07D213/74 ,  C07D213/75

    CPC classification number: C07D213/74 ,  C07D213/57 ,  C07D213/75

    Abstract: There are prepared compounds of the formula ##STR1## where R.sub.1 is halogen, R.sub.2 and R.sub.3 are hydrogen, halogen, trifluoromethyl, hydroxy, cyano, lower alkyl or lower alkoxy, R.sub.4 is hydrogen or lower alkyl, and R.sub.5 is hydrogen, lower alkyl, benzoyl, substituted benzoyl, lower carbalkoxy or ##STR2## where A is oxygen, sulfur, imino or lower alkylimino and R.sub.6 is lower alkyl, lower alkyl having 1 to 3 halogen atoms, lower alkenyl, hydroxymethyl, carboxymethyl, carb-lower alkoxy methyl, amino lower alkyl or alkylaminoalkyl having 2 to 13 carbon atoms or where any hydroxy or primary or secondary amino group is substituted by an alkanoyl group of 2 to 8 carbon atoms, carbalkoxy having 1 to 6 carbon atoms, carbophenoxy or carbobenzyloxy or a pharmacologically acceptable salt thereof. The compounds are useful in emotional disturbances, tension, anxiety, increased irritability.

    Abstract translation: 制备具有下式的化合物，其中R1是卤素，R2和R3是氢，卤素，三氟甲基，羟基，氰基，低级烷基或低级烷氧基，R4是氢或低级烷基，R5是氢，低级烷基， 苯甲酰基，取代的苯甲酰基，低级烷氧基或低级烷氧基，或其中A为氧，硫，亚氨基或低级烷基亚氨基，R6为低级烷基，具有1-3个卤素原子的低级烷基，低级烯基，羟甲基，羧甲基， 具有2至13个碳原子的氨基低级烷基或烷基氨基烷基或任何羟基或伯或仲氨基被2至8个碳原子的烷酰基取代，具有1至6个碳原子的烷氧基，碳苯氧基或苄氧羰基或药理学上可接受的盐 其中。 这些化合物可用于情绪障碍，紧张，焦虑，烦躁不安。

    2-Benzoyl-3-amino-pyridines
    28.
    发明授权
    2-Benzoyl-3-amino-pyridines 失效
    2-苯甲酰基-3-氨基 - 吡啶

    公开(公告)号：US3969361A

    公开(公告)日：1976-07-13

    申请号：US497750

    申请日：1974-08-15

    Applicant: Walter VON Bebenburg ,  Heribert Offermanns

    Inventor： Walter VON Bebenburg ,  Heribert Offermanns

    IPC: C07D213/75

    Abstract: There are prepared compounds of the formula ##SPC1##Where R.sub.1 is halogen, R.sub.2 and R.sub.3 are hydrogen, halogen, trifluoromethyl, hydroxy, cyano, lower alkyl or lower alkoxy, R.sub.4 is hydrogen or lower alkyl, and R.sub.5 is hydrogen, lower alkyl, benzoyl, substituted benzoyl, lower carbalkoxy or ##EQU1## where A is oxygen, sulfur, imino or lower alkylimino and R.sub.6 is lower alkyl, lower alkyl having 1 to 3 halogen atoms, lower alkenyl, hydroxymethyl, carboxymethyl, carb-lower alkoxy methyl, amino lower alkyl or alkylaminoalkyl having 2 to 13 carbon atoms or where any hydroxy or primary or secondary amino group is substituted by an alkanoyl group of 2 to 8 carbon atoms, carbalkoxy having 1 to 6 carbon atoms, carbophenoxy or carbobenzyloxy or a pharmacologically acceptable salt thereof. The compounds are useful in emotional disturbances, tension, anxiety, increased irritability.

    Abstract translation: 制备下式的化合物，其中R1是卤素，R2和R3是氢，卤素，三氟甲基，羟基，氰基，低级烷基或低级烷氧基，R4是氢或低级烷基，R5是氢，低级烷基，苯甲酰基，取代的 苯甲酰基，低级烷氧基或A并联-C-R6，其中A为氧，硫，亚氨基或低级烷基亚氨基，R6为低级烷基，具有1至3个卤素原子的低级烷基，低级烯基，羟甲基，羧甲基，碳 - 低级烷氧基甲基， 具有2至13个碳原子的氨基低级烷基或烷基氨基烷基或任何羟基或伯或仲氨基被2至8个碳原子的烷酰基取代，具有1至6个碳原子的烷氧基，碳苯氧基或苄氧羰基或药理学上可接受的盐 其中。 这些化合物可用于情绪障碍，紧张，焦虑，烦躁不安。

    Process of making penicillamine
    29.
    发明授权
    Process of making penicillamine 失效
    制作青霉胺的过程

    公开(公告)号：US3948984A

    公开(公告)日：1976-04-06

    申请号：US346825

    申请日：1973-03-29

    Applicant: Friedrich Asinger ,  Heribert Offermanns ,  Miklos Ghyczy

    Inventor： Friedrich Asinger ,  Heribert Offermanns ,  Miklos Ghyczy

    IPC: C07D277/06 ,  C07C99/10

    CPC classification number: C07D277/06

    Abstract: Penicillamine and its hydrochloride are made by reacting isobutyraldehyde with elemental sulfur or a sulfur-containing compound and with gaseous ammonia so as to form 2-isopropyl-5.5-dimethyl-thiazoline-.DELTA..sup.3, then reacting the latter compound with substantially anhydrous hydrogen cyanide so as to form the corresponding thiazolidine 4-carbonitrile, thereupon treating the latter compound with an excess of concentrated hydrochloric acid at an elevated temperature and separating the components of the mixture formed and recovering the penicillamine hydrochloride which may then be converted to the free D,L-penicillamine.

    Abstract translation: 青霉胺及其盐酸盐通过使异丁醛与元素硫或含硫化合物和气态氨反应形成2-异丙基-5-二甲基 - 噻唑啉-TATA 3，然后使后一种化合物与基本上无水的氰化氢反应制得。 为了形成相应的噻唑烷4-甲腈，随后在高温下用过量的浓盐酸处理后一种化合物，分离所形成的混合物的组分并回收盐酸青霉胺，然后将其转化为游离的D，L 青霉胺

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