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21. 发明授权

US4345100A Preparation of .alpha.-ketocarboxylic acid N-tert.-butylamides 失效
标题翻译： α-酮羧酸N-叔丁基酰胺的制备
公开(公告)号：US4345100A
公开(公告)日：1982-08-17
申请号：US222222
申请日：1981-01-02
申请人： Gerhard Bonse , Heinz U. Blank
发明人： Gerhard Bonse , Heinz U. Blank
IPC分类号： C07C231/06 , C07C67/00 , C07C231/00 , C07C235/72 , C07D253/075 , C07C102/08
CPC分类号： C07D253/075
摘要： A process for the preparation of an .alpha.-ketocarboxylic acid N-tert.-butylamide of the formulaR--CO--CO--NH--C(CH.sub.3).sub.3in whichR is an aliphatic radical with up to 8 carbon atoms, a cycloalkyl radical with 3 to 6 carbon atoms, a phenyl or naphthyl radical or a heterocyclic radical,comprising reacting an acyl cyanide of the formulaR--CO--CNwith tert.-butyl methyl ether of the formula(CH.sub.3).sub.3 C--O--CH.sub.3at a temperature between about 0.degree. and 80.degree. C. in the presence of an acid which is capable of activating the ether of formula (III) under the reaction conditions to give a tert.-butyl carbonium ion, and then hydrolyzing the reaction mixture. Advantageously the acyl cyanide is pivaloyl cyanide or benzoyl cyanide and is reacted with an approximately equimolar amount of the ether in the presence of about 1.1 to 1.5 times the molar amount of concentrated sulphuric acid as the activating acid. The products are useful as intermediates in the synthesis of known herbicides.
摘要翻译：制备式R-CO-CO-NH-C（CH3）3的α-酮羧酸N-叔丁基酰胺的方法，其中R是具有至多8个碳原子的脂族基团，环烷基具有3至6个碳原子，苯基或萘基或杂环基，其包括使式R-CO-CN的酰基氰与式（CH 3）3 C-O-CH 3的叔丁基甲基醚在在能够在反应条件下活化式（III）的醚的酸存在下，温度在约0℃至80℃之间，得到叔丁基碳鎓离子，然后水解反应混合物。有利地，酰基氰是新戊酰氰或苯甲酰氰，并且在作为活化酸的浓硫酸的摩尔量的约1.1至1.5倍的存在下，与约等摩尔量的醚反应。该产品可用作合成已知除草剂的中间体。

22. 发明授权

US4246279A Novel dichloromaleic acid diamide derivatives and their use as fungicides 失效
标题翻译：新型二氯马来酸二酰胺衍生物及其作为杀真菌剂的用途
公开(公告)号：US4246279A
公开(公告)日：1981-01-20
申请号：US8145
申请日：1979-01-31
申请人： Gerhard Bonse , Heinz U. Blank , Wilhelm Brandes , Paul Volker
发明人： Gerhard Bonse , Heinz U. Blank , Wilhelm Brandes , Paul Volker
IPC分类号： A01N37/18 , A01N37/22 , A01N37/30 , A01N43/16 , A01N47/02 , C07C67/00 , C07C233/09 , C07C233/15 , C07C233/20 , C07C233/27 , C07C233/38 , C07C253/00 , C07C255/29 , C07C313/00 , C07C323/41 , C07D307/52 , C07D309/04 , C07D309/20 , C07C103/58 , A01N9/20
CPC分类号： C07D309/04 , A01N37/22 , A01N37/30 , A01N43/16 , A01N47/02 , C07D307/52 , C07D309/20
摘要： Dichloromaleic acid diamides of the formula ##STR1## in which R represents an optionally substituted aliphatic radical with up to 8 carbon atoms, a cycloalkyl radical with 3 to 6 carbon atoms or a substituted phenyl radical,which possess fungicidal properties, are produced by reacting a dichloromaleic halide of the formula ##STR2## in which X is halogen,with an amine of the formulaH.sub.2 N--Rin a diluent and in the presence of an acid-binding agent.
摘要翻译：其中R表示具有至多8个碳原子的任选取代的脂肪族基团，具有3至6个碳原子的环烷基或具有杀真菌性质的取代苯基的式“IMAGE”的二氯苹果酸二酰胺通过使其中X是卤素的式“IMAGE”的二氯马来酰卤与式H2N-R的胺在稀释剂中并在酸结合剂的存在下反应。

23. 发明授权

US05998418A Enrofloxacine injection or infusion solutions 失效
标题翻译：恩氟沙星注射液或输注液
公开(公告)号：US05998418A
公开(公告)日：1999-12-07
申请号：US875061
申请日：1997-07-07
申请人： Gerhard Bonse , Martin Hamm , Hanns-Peter Muller , Arundev Haribhai Naik, deceased , Martin Scheer , Michael Stegemann , Oliver Vetter
发明人： Gerhard Bonse , Martin Hamm , Hanns-Peter Muller , Arundev Haribhai Naik, deceased , Martin Scheer , Michael Stegemann , Oliver Vetter
IPC分类号： A61K9/08 , A61K31/19 , A61K31/495 , A61K31/70 , A61K47/12 , A61K47/18 , A61K47/26 , A61K47/42
CPC分类号： A61K31/496 , A61K31/7004 , A61K47/12 , A61K47/183 , A61K47/26 , A61K9/0019
摘要： The present invention relates to novel injection and infusion solutions of the following composition:a) 0.1 to 20% by weight of enrofloxacin, based on the total weight of the solution, in the form of its salts with polyhydroxycarboxylic acids or amino acids or mixtures thereof,b) polyhydroxycarboxylic acids, amino acids or mixtures thereof in 0.1 to 5 molar excess, based on enrofloxacin;c) optionally 0.1 to 30% by weight of formulation aids, based on the total weight of the solution;d) water to 100% by weight.
摘要翻译： PCT No.PCT / EP95 / 05147 371日期1997年7月7日 102（e）日期1997年7月7日PCT 1995年12月28日PCT PCT。公开号WO96 / 21453 日本1996年7月18日本发明涉及以下组合物的新型注射和输注溶液：a）以其与多羟基羧酸的盐形式的0.1至20重量％的恩氟沙星，基于溶液的总重量，氨基酸或其混合物，b）基于恩氟沙星的0.1-5摩尔过量的聚羟基羧酸，氨基酸或其混合物; c）任选地0.1至30重量％的制剂助剂，基于溶液的总重量; d）水至100重量％。

24. 发明授权

US4980479A Preparation of novel 5-acyloxy-4 (5H)-oxazolonium salts suited for use as intermediates for triazinone herbicides 失效
标题翻译：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：US4980479A
公开(公告)日：1990-12-25
申请号：US427162
申请日：1989-10-25
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
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--N (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.

25. 发明授权

US4804655A Pesticidal cyclic malonylphosphonic diamides 失效
标题翻译：杀虫环丙二酸二酰胺
公开(公告)号：US4804655A
公开(公告)日：1989-02-14
申请号：US945442
申请日：1986-12-22
申请人： Nikolaus Muller , Gerhard Bonse , Peter Andrews , Wilhelm Stendel , Robert Steffens
发明人： Nikolaus Muller , Gerhard Bonse , Peter Andrews , Wilhelm Stendel , Robert Steffens
IPC分类号： A01N57/36 , C07F9/6584 , C07F9/22
CPC分类号： C07F9/65848 , A01N57/36
摘要： Novel pesticidally active cyclic malonylphosphonic diamides of the formula ##STR1## in which X.sup. represents O or S,R.sup.1 represents alkyl, alkenyl, alkinyl, cycloalkyl, aryl or heteroaryl, each of which can be optionally substituted,R.sup.2 represents hydrogen, alkyl, aryl or aralkyl,R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, andR.sup.4 represents an acyl radical,or salts thereof, Many intermediates are new,
摘要翻译：式中，X代表O或S，R1代表烷基，链烯基，炔基，环烷基，芳基或杂芳基，其中每一个可任选被取代的式“IMAGE”的新型杀虫活性环丙二酸膦酰二酰胺，R2代表氢，烷基，芳基或芳烷基，R 3表示氢，烷基，芳基或芳烷基，R 4表示酰基，或其盐。许多中间体是新的，

26. 发明授权

US4456769A Preparation of hydrazidines 失效
标题翻译：肼的制备
公开(公告)号：US4456769A
公开(公告)日：1984-06-26
申请号：US387906
申请日：1982-06-14
申请人： Gerhard Bonse , Thomas Schmidt
发明人： Gerhard Bonse , Thomas Schmidt
IPC分类号： A01N43/64 , C07C20060101 , C07C67/00 , C07C239/00 , C07C257/22 , C07D20060101 , C07C123/02
CPC分类号： C07C257/22
摘要： A new one-step process for the preparation of hydrazidines of the general formula ##STR1## in which R represents an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group or an optionally substituted aralkyl group,or their acid addition salts, in high yield comprises reacting iminoalkyl ethers of the general formula ##STR2## in which R has the abovementioned meaning andR.sup.1 represents an optionally substituted alkyl group or an optionally substituted cycloalkyl group,or their acid addition salts, with hydrazine in solvents under reduced pressure and at temperatures between -80.degree. and +100.degree. C., the reaction being effected in the presence of water present in the solvent and/or in the hydrazine by employing it as hydrazine hydrate. The hydrazidines of formula (I) and their salts are valuable intermediates in heterocyclic chemistry, for example for the synthesis of herbicidally active as-triazinones.
摘要翻译：制备通式为（I）的肼的新的一步法，其中R表示任选取代的烷基，任选取代的环烷基，任选取代的芳基或任选取代的芳烷基，或它们的高收率的酸加成盐包括使通式为其中R具有上述含义并且R 1表示任选取代的烷基或任选取代的环烷基的通式为其中的亚氨基烷基醚或其酸加成盐，用肼在溶剂中在减压下和-80℃至+ 100℃的温度下进行，反应在存在于溶剂和/或肼中的水存在下通过将其用作水合肼来进行。式（I）的肼及其盐是杂环化学中的有价值的中间体，例如合成除草活性的三嗪酮。

27. 发明授权

US4443629A Preparation of hydrazidines 失效
标题翻译：肼的制备
公开(公告)号：US4443629A
公开(公告)日：1984-04-17
申请号：US387907
申请日：1982-06-14
申请人： Gerhard Bonse , Thomas Schmidt
发明人： Gerhard Bonse , Thomas Schmidt
IPC分类号： A01N43/707 , A01N43/64 , C07C20060101 , C07C67/00 , C07C239/00 , C07C257/22 , C07C123/02
CPC分类号： C07C257/22
摘要： A one-step process for the preparation of hydrazidines of the general formula ##STR1## in which R represents an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted aryl group or an optionally substituted aralkyl group, or their acid addition salts, in high yield, comprises reacting appropriate amidines or their acid addition salts with hydrazine in solvents at reduced pressure and at temperatures between -80.degree. C. and +100.degree. C., the reaction being effected in the presence of water present in the solvent and/or in the hydrazine by employing it as hydrazine hydrate. The hydrazidines of formula (I) and their salts are valuable intermediates in heterocyclic chemistry, for example for the synthesis of herbicidally active as-triazinones.
摘要翻译：制备通式为（I）的肼的一步法，其中R表示任选取代的烷基，任选取代的环烷基，任选取代的芳基或任选取代的芳烷基，或它们的高收率的酸加成盐包括使适当的脒或其酸加成盐与肼在减压和-80℃至+ 100℃的温度下在溶剂中反应，反应在存在水的情况下进行在溶剂和/或肼中通过将其用作水合肼。式（I）的肼及其盐是杂环化学中的有价值的中间体，例如合成除草活性的三嗪酮。

28. 发明授权

US4328340A Preparation of 4-amino-6-tert.-butyl-3-alkylthio-1,2,4-triazin-5-(4H)-ones 失效
标题翻译：制备4-氨基-6-叔丁基-3-烷硫基-1,2,4-三嗪-5-（4H） - 酮
公开(公告)号：US4328340A
公开(公告)日：1982-05-04
申请号：US235496
申请日：1981-02-19
申请人： Gerhard Bonse , Heinz U. Blank , Hans Kratzer
发明人： Gerhard Bonse , Heinz U. Blank , Hans Kratzer
IPC分类号： C07D253/06 , C07D253/075
CPC分类号： C07D253/075
摘要： In the preparation of 4-amino-6-tert.-butyl-3-methylthio-1,2,4-triazin-5-(4H)-one of the formula ##STR1## wherein pivaloyl cyanide of the formula(CH.sub.3).sub.3 C--CO--CNis reacted to form an intermediate, the intermediate is condensed with thiocarbohydrazide of the formulaNH.sub.2 --NH--CS--NH--NH.sub.2to form 4-amino-6-tert.-butyl-3-mercapto-1,2,4-triazin-5-(4H)-one of the formula ##STR2## and the 4-amino-6-tert.-butyl-3-mercapto-1,2,4-triazin-5-(4H)-one is alkylated to replace the H atom on the sulphur by --C.sub.1-4 --alkyl, the improvement which comprises reacting the pivaloyl cyanide with a carboxylic acid anhydride of the formulaR--CO--O--CO--Rin which R is an optionally substituted aliphatic radical with up to 8 carbon atoms or an optionally substituted phenyl radical, in the presence of a strong acid at a temperature between about -50.degree. and +150.degree. C., and then directly reacting the reaction mixture thus obtained with the thiocarbahydrazide. Advantageously R is CH.sub.3, the strong acid is concentrated sulphuric acid, the pivaloyl cyanide is effected at a temperature between about 0.degree. and 100.degree. C., the condensation with thiocarbohydrazide is effected, in the presence of a mineral acid, in an aqueous or aqueous-alcoholic medium, and the alkylation is effected using methyl iodide or methyl bromide in the presence of sodium hydroxide at about 0.degree. to 50.degree. C.
摘要翻译：在制备式（CH 3）3 C的新戊酰基氰的4-氨基-6-叔丁基-3-甲硫基-1,2,4-三嗪-5-（4H） - 酮中， -CO-CN反应形成中间体，中间体与式NH 2 -NH-CS-NH-NH 2的硫代碳酰肼缩合形成4-氨基-6-叔丁基-3-巯基-1,2，（4H） - 酮和4-氨基-6-叔丁基-3-巯基-1,2,4-三嗪-5-（4H） - 酮是烷基化以用-C 1-4烷基取代硫上的H原子，其改进包括使新戊酰氰与式R-CO-O-CO-R的羧酸酐反应，其中R是任选取代的脂族具有多达8个碳原子的基团或任选取代的苯基，在强酸存在下，在约-50至+ 150℃之间的温度下，然后将由此获得的反应混合物与硫代碳酰肼直接反应。有利地，R是CH 3，强酸是浓硫酸，新戊酰氰在约0℃至100℃的温度下进行，与硫代碳酰肼的缩合在无机酸的存在下，在水或水性醇介质，在氢氧化钠存在下，在约0〜50℃下，使用甲基碘或甲基溴进行烷基化。

29. 发明授权

US4279921A Dichloromaleic acid diamide derivatives and their use as fungicides 失效
标题翻译：二氯马来酸二酰胺衍生物及其作为杀真菌剂的用途
公开(公告)号：US4279921A
公开(公告)日：1981-07-21
申请号：US123868
申请日：1980-02-22
申请人： Gerhard Bonse , Heinz U. Blank , Wilhelm Brandes , Volker Paul
发明人： Gerhard Bonse , Heinz U. Blank , Wilhelm Brandes , Volker Paul
IPC分类号： A01N37/18 , A01N37/22 , A01N37/30 , A01N43/16 , A01N47/02 , C07C67/00 , C07C233/09 , C07C233/15 , C07C233/20 , C07C233/27 , C07C233/38 , C07C253/00 , C07C255/29 , C07C313/00 , C07C323/41 , C07D307/52 , C07D309/04 , C07D309/20 , A01N43/08 , C07D307/54 , C07D309/32
CPC分类号： C07D309/04 , A01N37/22 , A01N37/30 , A01N43/16 , A01N47/02 , C07D307/52 , C07D309/20
摘要： The present invention relates to dichloromaleic acid diamides of the formula ##STR1## in which R represents an optionally substituted aliphatic radical with up to 8 carbon atoms, a cycloalkyl radical with 3 to 6 carbon atoms or a substituted phenyl radical which possess fungicidal properties and are produced by reacting a dichloromaleic acid halide of the formula ##STR2## in which X is halogen with an amine of the formulaH.sub.2 N--Rin a diluent and in the presence of an acid-binding agent.
摘要翻译：本发明涉及式“IMAGE”的二氯马来酸二酰胺，其中R表示任选取代的具有至多8个碳原子的脂族基团，具有3至6个碳原子的环烷基或具有杀真菌性质的取代苯基，通过在稀释剂中和在酸结合剂的存在下，使式（XI）中X为卤素的二氯马来酰卤与式H2N-R的胺反应而制得。

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