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    Method for the production of ivermectin
    2.
    发明授权
    Method for the production of ivermectin 失效
    生产伊维菌素的方法

    公开(公告)号：US6072052A

    公开(公告)日：2000-06-06

    申请号：US297241

    申请日：1999-04-27

    申请人： Dieter Arlt ,  Gerhard Bonse

    发明人： Dieter Arlt ,  Gerhard Bonse

    IPC分类号： C07H17/08 ,  C07H19/01

    CPC分类号： C07H17/08

    摘要： The present invention relates to a process for preparing ivermectin by selective hydrogenation of avermectin and subsequent removal of the catalyst.

    摘要翻译： PCT No.PCT / EP97 / 05777 一九九九年四月二十七日 102（e）日期1999年4月27日PCT 1997年10月20日PCT公布。 公开号WO98 / 18806 日期1998年5月7日本发明涉及通过阿维菌素的选择性氢化和随后除去催化剂来制备伊维菌素的方法。

    Preparation of novel 5-acyloxy-4-(5H)-oxazolonium salts suited for use as intermediates for triazinone herbicides
    3.
    发明授权
    Preparation of novel 5-acyloxy-4-(5H)-oxazolonium salts suited for use as intermediates for triazinone herbicides 失效
    制备适合用作三嗪酮除草剂的中间体的新型5-酰氧基-4-（5H） - 恶唑鎓盐

    公开(公告)号：US4594427A

    公开(公告)日：1986-06-10

    申请号：US360495

    申请日：1982-03-22

    申请人： Gerhard Bonse ,  Gerhard Marzolph ,  Heinz U. Blank

    发明人： Gerhard Bonse ,  Gerhard Marzolph ,  Heinz U. Blank

    IPC分类号： C07D253/06 ,  C07D253/075 ,  C07D263/44 ,  C07D413/04 ,  C07D263/08 ,  C07D285/08

    CPC分类号： C07D253/075 ,  C07D263/44

    摘要： Novel 5-acyloxy-4(5H)-oxazolonium salts of the formula ##STR1## in which R.sup.1 represents an optionally substituted aliphatic group with up to 12 carbon atoms, an optionally substituted cycloalkyl group with 3 to 10 carbon atoms, an optionally substituted phenyl or naphthyl group or an optionally substituted heterocyclic group andR.sup.2 and R.sup.3 are identical or different and represent a hydrogen atom or an optionally substituted aliphatic group with up to 8 carbon atoms or an optionally substituted phenyl group andX.sup..crclbar. represents the anion of an inorganic or organic acid having a pK.sub.a value of less than 2,are obtained in solution when an acyl cyanide of the general formulaR.sup.1 --CO--CN (II)is reacted with a carboxylic acid anhydride of the general formulaR.sup.2 --CO--O--CO--R.sup.3 (III)whereinR.sup.1, R.sup.2 and R.sup.3 each have the abovementioned meaning,in the presence of one or more inorganic or organic acids having a pK.sub.a value of less than 2, and if appropriate in the presence of a solvent, and if appropriate at a temperature between 0.degree. and 120.degree. C.The novel oxazolonium salts (I) can be used as intermediate products for the preparation of known, herbicidally active 3,4,6-trisubstituted 1,2,4-triazin-5(4H)-ones.

    摘要翻译： 式（Ⅰ）的新的5-酰氧基-4（5H） - 恶唑盐，其中R 1表示任选取代的具有至多12个碳原子的脂族基团，任选取代的具有3至10个碳原子的环烷基， 任选取代的苯基或萘基或任选取代的杂环基，R2和R3相同或不同，表示氢原子或任选取代的具有至多8个碳原子的脂族基团或任选取代的苯基，X（ - ）表示 当通式R 1 -CO-CN（II）的酰基氰与通式为R 2 -CO的羧酸酐反应时，溶液中得到pKa值小于2的无机或有机酸的阴离子 在一种或多种pKa值小于2的无机或有机酸的存在下，并且如果在溶剂存在下适当，其中R 1，R 2和R 3各自具有上述含义的-O-CO-R 3（III） ，如果合适的话 在0至120℃之间的温度下，新的恶唑鎓盐（I）可用作中间产物，用于制备已知的除草活性的3,4,6-三取代的1,2,4-三嗪-5（4H ）-那些。

    Preparation of 4-methyl-5-oxo-3-thioxo-tetrahydro-1,2,4,-(2H,4H)-triazines
    4.
    发明授权
    Preparation of 4-methyl-5-oxo-3-thioxo-tetrahydro-1,2,4,-(2H,4H)-triazines 失效
    制备4-甲基-5-氧代-3-硫代 - 四氢-1,2,4 - （2H，4H） - 三嗪

    公开(公告)号：US4436905A

    公开(公告)日：1984-03-13

    申请号：US406679

    申请日：1982-08-09

    申请人： Gerhard Bonse

    发明人： Gerhard Bonse

    IPC分类号： C07D253/06 ,  A01N43/707 ,  C07D253/075

    CPC分类号： C07D253/075

    摘要： 4-Methyl-5-oxo-3-thioxo-tetrahydro-1,2,4-(2H,4H)-triazines, which are intermediate products for known herbicides, can be prepared in high yields by a process in which an acyl cyanide of the general formulaR--CO--CN (II)wherein R represents an optionally substituted aliphatic radical having up to 12 carbon atoms, an optionally substituted cycloalkyl radical having 3 to 10 carbon atoms, an optionally substituted phenyl or naphthyl radical or an optionally substituted heterocyclic radical,is reacted with a carboxylic acid anhydride of the general formulaR.sup.1 --CO--O--CO--R.sup.1 (II)in which R.sup.1 represents an optionally substituted aliphatic radical having up to 8 carbon atoms or an optionally substituted phenyl radical,in the presence of a strong acid and, if appropriate, in the presence of a solvent, at a temperature between -50.degree. and 150.degree. C., and the reaction mixture thus obtained is then reacted directly with 4-methyl-thiosemicarbazide (CH.sub.3 --NH--CS--NH--NH.sub.2).

    摘要翻译： 作为已知除草剂的中间产物的4-甲基-5-氧代-3-硫代 - 四氢-1,2,4-（2H，4H） - 三嗪可以通过其中酰基氰化物 通式R-CO-CN（II）其中R表示任选取代的具有至多12个碳原子的脂族基团，任选取代的具有3-10个碳原子的环烷基，任选取代的苯基或萘基或任选取代的 杂环基与通式R 1 -CO-O-CO-R 1（II）的羧酸酐反应，其中R 1表示任选取代的具有至多8个碳原子的脂族基团或任选取代的苯基，在 存在强酸，如果合适的话，在溶剂存在下，在-50℃和150℃之间，然后将所得反应混合物直接与4-甲基硫代氨基脲（CH 3 -NH） -CS-NH-NH 2）。

    Preparation of 3,6-disubstituted 4-amino-1,2,4-triazin-5-ones
    5.
    发明授权
    Preparation of 3,6-disubstituted 4-amino-1,2,4-triazin-5-ones 失效
    3,6-二取代的4-氨基-1,2,4-三嗪-5-酮的制备

    公开(公告)号：US4408044A

    公开(公告)日：1983-10-04

    申请号：US338811

    申请日：1982-01-11

    申请人： Thomas Schmidt ,  Helmut Timmler ,  Gerhard Bonse ,  Heinz U. Blank ,  Gerhard Marzolph

    发明人： Thomas Schmidt ,  Helmut Timmler ,  Gerhard Bonse ,  Heinz U. Blank ,  Gerhard Marzolph

    IPC分类号： C07D253/06 ,  A01N43/707 ,  C07D253/07 ,  C07D405/04 ,  C07D409/04

    CPC分类号： C07D253/065 ,  C07D253/07

    摘要： The herbicidal 3,6-substituted 4-amino-1,2,4-triazin-5-one of the general formula ##STR1## wherein R.sup.1 and R.sup.2 have the meaning given in the description,is obtained in good yields by a new two-stage cyclization reaction if an .alpha.-ketocarboxylic acid amide of the general formulaR.sup.1 --CO--CO--NHR.sup.3 (II)is reacted with a hydrazidine of the general formula ##STR2## if appropriate in the presence of a diluent at temperatures between 0.degree. and 150.degree. C., whereby in the first process stage a condensation reaction takes place to give condensation products which still have open chains, and in the second process stage an elimination reaction with ring closure takes place to give the end product of formula (I).

    摘要翻译： 通过以下方式获得通式（I）的除草3,6-取代的4-氨基-1,2,4-三嗪-5-酮，其中R1和R2具有说明书中给出的含义，以良好的产率由 如果通式为R 1 -CO-CO-NHR 3（II）的α-酮羧酸酰胺与通式为（III）的肼反应，则在适当的情况下，在 稀释剂在0℃至150℃的温度下进行，由此在第一工艺阶段进行缩合反应以产生仍具有开链的缩合产物，并且在第二工艺阶段中进行具有闭环的消除反应，以产生 式（I）的最终产物。

    Substituted 1,3,4-thiadizaolinones, processes for their preparation, and their use for combating endoparasites
    6.
    发明授权
    Substituted 1,3,4-thiadizaolinones, processes for their preparation, and their use for combating endoparasites 失效
    取代1,3,4-噻唑烷酮，其制备方法及其用于组合内生菌的用途

    公开(公告)号：US5095024A

    公开(公告)日：1992-03-10

    申请号：US581934

    申请日：1990-09-13

    申请人： Nikolaus Muller ,  Gerhard Bonse ,  Werner Lindner ,  Achim Harder

    发明人： Nikolaus Muller ,  Gerhard Bonse ,  Werner Lindner ,  Achim Harder

    IPC分类号： A01N43/824 ,  A61K31/41 ,  A61K31/433 ,  A61P33/00 ,  A61P33/10 ,  C07C243/28 ,  C07C337/02 ,  C07C337/06 ,  C07D285/12 ,  C07D285/125 ,  C07D285/13

    CPC分类号： C07D285/13 ,  C07C337/02 ,  C07D285/125

    摘要： Substituted 1,3,4-thiadiazolinones of the formula (I), ##STR1## in which X represents O or S,R.sup.1 represents hydrogen, alkyl, alkoxy, alkylthio, halogen, halogenoalkyl, halogenoalkoxy or halogenoalkylthio,R.sup.2 represents one or more identical or different radicals from the series comprising hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy and arylthio, each of which can, in turn, be substituted as well, andR.sup.3 represents alkyl, alkenyl or alkynyl, each of which can optionally be substituted,with the exception of the compound 5-methylmercapto-3-phenyl-1,3,4-thiadiazol-2-(3H)-one, are disclosed as being useful to combat endoparasites. Compositions containing these compounds, process for preparing them, and novel intermediates are also disclosed.

    摘要翻译： 取代的式（I）的1,3,4-噻二唑啉酮，其中X代表O或S，R1代表氢，烷基，烷氧基，烷硫基，卤素，卤代烷基，卤代烷氧基或卤代烷硫基，R2代表一 或更多相同或不同的基团，其包含氢，烷基，烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，亚烷基二氧基，卤代亚烷基二氧基，卤素，CN，NO 2，NH 2，烷基氨基，二烷基氨基，烷基羰基，烷氧基，烷基磺酰基，芳基磺酰基，氨磺酰基， 烷基氨磺酰基，二烷基氨磺酰基，芳基，芳氧基和芳硫基，其中每一个也可以被取代，并且R 3表示烷基，烯基或炔基，其中每一个可任选被取代，除了化合物5-甲基巯基 - 3-苯基-1,3,4-噻二唑-2-（3H） - 酮被公开用于对抗内寄生虫。 还公开了含有这些化合物的组合物，其制备方法和新型中间体。

    Process for the preparation of 1-amino-1,3,5-triazine-2,4(1H,3H)-diones
    7.
    发明授权
    Process for the preparation of 1-amino-1,3,5-triazine-2,4(1H,3H)-diones 失效
    1-氨基-1,3,5-三嗪-2,4（1H，3H） - 二酮的制备方法

    公开(公告)号：US4524205A

    公开(公告)日：1985-06-18

    申请号：US544334

    申请日：1983-10-21

    申请人： Gerhard Bonse ,  Reinhard Lantzsch ,  Henning Dorr ,  Wolfgang Kreiss ,  Karlfried Dickore ,  Klaus Ditgens ,  Eckart Kranz

    发明人： Gerhard Bonse ,  Reinhard Lantzsch ,  Henning Dorr ,  Wolfgang Kreiss ,  Karlfried Dickore ,  Klaus Ditgens ,  Eckart Kranz

    IPC分类号： A01N43/64 ,  C07D213/20 ,  C07D251/38 ,  C07D251/26

    CPC分类号： C07D213/20 ,  A01N43/64 ,  C07D251/38

    摘要： A process for the preparation of a herbicidally active 1-amino-1,3,5-triazone-2,4 (1H,3H)-dione of the formula ##STR1## comprising in a first stage at a temperature from about 0.degree. to 100.degree. C. reacting an isocyanate of the formulaR.sup.1 - NCO (II)with an isothio semicarbazone of the tautomeric formulas ##STR2## in which R.sup.3 and R.sup.4 each independently is hydrogen, alkyl, cycloalkyl, aralkyl o alkyl, cycloalkyl, aralkyl or aryl,thereby to form a urea derivative of the tautomeric formulas ##STR3## in a second stage at a temperature between about -50.degree. and 0.degree. C. reacting the urea derivative with phosgene (COCl.sub.2) in the presence of an auxiliary organic base and in the presence of a diluent, at least about 2 mols of phosgene and at least about 2 mols of the auxiliary base being used per mol of urea derivative, thereby to form a 1-alkylideneamino-1,3,5-triazine-2,4(1H,3H)-dione of the formula V ##STR4## and in a third stage converting the 1-alkylideneamino group to a 1-amino group.

    摘要翻译： 制备式（I）的除草活性1-氨基-1,3,5-三嗪-2,4（1H，3H） - 二酮的方法，其包含在第一阶段中在约 使式R 1 -NCO（II）的异氰酸酯与互变异构结构式（III）的异噻唑烷酮反应，其中R 3和R 4各自独立地为氢，烷基，环烷基，芳烷基烷基 ，环烷基，芳烷基或芳基，从而在约-50℃至0℃的温度下在第二阶段中形成互变异构体式（IV）的脲衍生物。将脲衍生物与光气（COCl 2）在 辅助有机碱的存在和在稀释剂存在下，每摩尔脲衍生物使用至少约2摩尔的光气和至少约2摩尔的辅助碱，从而形成1-亚烷基氨基-1， （V）的3,5-三嗪-2,4（1H，3H） - 二酮，在第一阶段将1-亚烷基氨基转化为1-氨基 没有组。

    Use of benzimidazole derivatives as yield promoters
    9.
    发明授权
    Use of benzimidazole derivatives as yield promoters 失效
    苯并咪唑衍生物作为产率促进剂的应用

    公开(公告)号：US4960783A

    公开(公告)日：1990-10-02

    申请号：US292581

    申请日：1988-12-30

    申请人： Gerhard Bonse ,  Werner Hallenbach ,  Hans Lindel ,  Friedrich Berschauer

    发明人： Gerhard Bonse ,  Werner Hallenbach ,  Hans Lindel ,  Friedrich Berschauer

    IPC分类号： A23K1/16 ,  C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/26

    CPC分类号： C07D235/06 ,  C07D235/08 ,  C07D235/10 ,  C07D235/26

    摘要： Method of promoting the yield and growth of animals which comprises administering to such animals a yield and growth promoting effective amount of a benzimidazole derivative of the formula ##STR1## in which R.sup.1 stands for hydrogen, hydroxyl, alkyl or halogenoalkyl,R.sup.2 stands for hydrogen, alkyl, halogen, CN or halogenalkyl,R.sup.3 stands for hydrogen, alkyl or acyl,R.sup.4 stands for hydrogen, alkyl or halogenoalkyl,R.sup.5 stands for alkyl or halogenoalkyl,R.sup.6 stands for alkyl or cycloalkyl, which is optionally substituted by halogen, cycloalkyl, OH, alkoxy, halogenoalkoxy or aryl, which can in turn be substituted by alkyl, halogen, CN or the radicals --COR.sup.7, --O--alkylene--COR.sup.7, --alkylene--R.sup.8 or --O-- alkylene--R.sup.8,R.sup.7 stands for hydroxyl, alkoxy or --NR.sup.9 R.sup.10,R.sup.8 stands for hydroxyl, alkoxy or --NR.sup.9 R.sup.10,R.sup.9 stands for hydrogen or alkyl andR.sup.10 stands for hydrogen or alkyl,or physiologically tolerated salts thereof. The active materials are new except for those in whichR.sup.1 stands for hydrogen,R.sup.4 stands for hydrogen,R.sup.5 stands for methyl andR.sup.6 stands for methyl.

    摘要翻译： 促进动物产量和生长的方法，其包括向所述动物施用产量和生长促进有效量的式（I）的苯并咪唑衍生物，其中R1代表氢，羟基，烷基或卤代烷基，R2代表 对于氢，烷基，卤素，CN或卤代烷基，R3代表氢，烷基或酰基，R4代表氢，烷基或卤代烷基，R5代表烷基或卤代烷基，R6代表烷基或环烷基， 环烷基，OH，烷氧基，卤代烷氧基或芳基，其又可以被烷基，卤素，CN或基团-COR7，-O-亚烷基-COR7， - 亚烷基-R8或-O-亚烷基-R8取代，R7代表 羟基，烷氧基或-NR9R10，R8代表羟基，烷氧基或-NR9R10，R9代表氢或烷基，R10代表氢或烷基或其生理上耐受的盐。 活性物质是新的，除了其中R1代表氢，R4代表氢，R5代表甲基，R6代表甲基的那些。