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    Process for the production of substituted pyridine (A)
    5.
    发明授权
    Process for the production of substituted pyridine (A) 失效
    制备取代吡啶（A）的方法

    公开(公告)号：US4175195A

    公开(公告)日：1979-11-20

    申请号：US830984

    申请日：1977-09-06

    申请人： Helmut Beschke ,  Heinz Friedrich ,  Heribert Offermanns

    发明人： Helmut Beschke ,  Heinz Friedrich ,  Heribert Offermanns

    IPC分类号： C07D213/12 ,  C07D213/22 ,  C07D405/04 ,  C07D409/04

    CPC分类号： C07D213/22 ,  C07D213/12

    摘要： Pyridines substituted in the 2-position by an aromatic or heteroaromatic group are prepared by reacting an aliphatic aromatic or aliphatic heteroaromatic ketone with an aliphatic oxo compound having a carbon to carbon ethylenic double bond on the carbon atom adjacent to the oxo group and ammonia in the presence of a dehydrating and dehydrogenating catalyst at a temperature of about 250.degree. to 550.degree. C.

    摘要翻译： 通过芳族或杂芳族基团在2位上取代的吡啶通过使脂族芳族或脂族杂芳族酮与在与氧代基相邻的碳原子上具有碳 - 碳烯键式双键的脂族氧代化合物和氨在 在约250℃至550℃的温度下存在脱水和脱氢催化剂。

    Process of making penicillamine
    6.
    发明授权
    Process of making penicillamine 失效
    制作青霉胺的过程

    公开(公告)号：US4060548A

    公开(公告)日：1977-11-29

    申请号：US642572

    申请日：1975-12-19

    申请人： Friedrich Asinger ,  Heribert Offermanns ,  Miklos Ghyczy

    发明人： Friedrich Asinger ,  Heribert Offermanns ,  Miklos Ghyczy

    IPC分类号： C07D277/06 ,  C07C99/10

    CPC分类号： C07D277/06

    摘要： Penicillamine and its hydrochloride are made by reacting i-butyraldehyde 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.

    摘要翻译： 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氢 氰化物以形成相应的噻唑烷-4-腈，然后在升高的温度下用过量的浓盐酸处理后一化合物，并分离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D ，L-青霉胺。

    6-Aza-3H-1,4-benzodiazepines
    7.
    发明授权
    6-Aza-3H-1,4-benzodiazepines 失效
    6-氮杂-3H-1,4-苯并二氮杂

    公开(公告)号：US4008223A

    公开(公告)日：1977-02-15

    申请号：US507605

    申请日：1974-09-19

    申请人： Walter Von Bebenburg ,  Heribert Offermanns

    发明人： Walter Von Bebenburg ,  Heribert Offermanns

    IPC分类号： C07D471/04

    摘要： There are produced 6-aza-3H-1, 4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula ##STR1## where R.sub.1 is a halogen, R.sub.2 and R.sub.3 are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl, lower alkoxy, R.sub.4 is hydrogen, hydroxyl, hydroxyl acylated with a mono or dicarboxylic aid of 2 to 6 carbon atoms, lower alkoxy, lower alkyl, benzyl, lower aliphatic acyl, carboxy or carb-lower alkoxy, Z is nitrogen or NO, R.sub.5 is hydrogen, lower alkyl, lower alkyl substituted with cycloalkyl of 3 to 6 carbon atoms, lower alkenyl, cycloalkyl of 3 to 6 carbon atoms , lower hydroxyalkyl, benzyl, aliphatic acyl of 2 to 6 carbon atoms aminoalkyl of 2 to 7 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 7 carbon atoms, lower alkyl substituted with 5 to 7 membered N-heterocyclic ring, containing 0 to 1 additional nitrogen or oxygen atoms, and A is oxygen, sulfur, =NR.sub.5, =NOR.sub.5, =NH-NHR.sub.5 or two hydrogen atoms and the --N(R.sub.5)--C--(=A)-- can also be in the tautomeric form --N=C(AR.sub.5) 13 and pharmacologically acceptable salts thereof. The compounds have spasmolytic, antiphlogistic and tranquilizer activity.

    摘要翻译： 产生式“IMAGE”的6-氮杂-3H-1,4-苯并二氮杂和6-氮杂-1,2-二氢-3H-1,4-苯并二氮杂其中R 1是卤素，R 2和R 3是氢， 卤素，三氟甲基，硝基，腈，羟基，低级烷基，低级烷氧基，R 4是氢，羟基，用2至6个碳原子的单或二羧酸酰化的羟基，低级烷氧基，低级烷基，苄基，低级脂族酰基，羧基 或碳 - 低级烷氧基，Z为氮或NO，R5为氢，低级烷基，被3至6个碳原子的环烷基取代的低级烷基，低级烯基，3至6个碳原子的环烷基，低级羟基烷基，苄基，脂族酰基 2至6个碳原子，2至7个碳原子的氨基烷基，2至7个碳原子的一或二低级烷基取代的氨基烷基，由5至7元N-杂环取代的低级烷基，含有0至1个额外的氮或氧原子， 并且A是氧，硫，= NR5，= NOR5，= NH-NHR5或两个氢原子，-N（R5）-C-（= A） - 也可以是τ 多晶型-N = C（AR5）13及其药理学上可接受的盐。 这些化合物具有解痉，消炎和镇静作用。

    Process for the production of thiazolines-(3)
    8.
    发明授权
    Process for the production of thiazolines-(3) 失效
    生产噻唑啉的方法 - （3）

    公开(公告)号：US3931208A

    公开(公告)日：1976-01-06

    申请号：US413048

    申请日：1973-11-05

    申请人： Heribert Offermanns ,  Friedrich Asinger ,  Wolf-Dieter Pfeifer ,  Paul Scherberich ,  Gerd Schreyer

    发明人： Heribert Offermanns ,  Friedrich Asinger ,  Wolf-Dieter Pfeifer ,  Paul Scherberich ,  Gerd Schreyer

    IPC分类号： C07D277/10 ,  C07D277/60

    CPC分类号： C07D277/60 ,  C07D277/10

    摘要： 2 AND 5 SUBSTITUTED THIAZOLINE-(3) COMPOUNDS OF THE FORMULA: ##EQU1## in which R.sub.1, R.sub.2, and R.sub.3 and R.sub.4 are the same or different, R.sub.1 and R.sub.2 are straight or branched chain lower alkyl, alkenyl or aralkyl groups or together are a straight or branched chain alkylene or ethylenically unsaturated divalent aliphatic hydrocarbon group which joins with the adjacent carbon atom to form a ring and R.sub.3 and R.sub.4 are similarly defined except R.sub.3 can also be hydrogen by reaching a 2,2' dioxodisulfide of the formula ##EQU2## with an oxo compound of the formula ##EQU3## and with ammonia and hydrogen sulfide in the presence of an amine and an ammonium salt.

    摘要翻译： 2和5取代的噻唑啉 - （3）式的化合物：其中R 1，R 2和R 3和R 4相同或不同，R 1和R 2是直链的 或支链低级烷基，烯基或芳烷基或一起是与相邻碳原子连接以形成环的直链或支链亚烷基或烯键式不饱和二价脂族烃基，并且R 3和R 4类似地定义，除了R 3也可以是氢 通过到达式OO C的二氧杂二硫化物。方法C将C 1 -C 6（C 1 -C 6）环烷基（R 2）R 2 R 2与式R 3的氧代化合物反应。 和氨和硫化氢在胺和铵盐的存在下反应。

    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

    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。