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1. 发明授权

US4789746A Process for the preparation of the (+)-antipode of (E)-1-cyclohexyl-4,4-dimethyl-3-hydroxy-2-(1,2,4-triazol-1-yl)-pent-1-en e 失效
标题翻译：（E）-1-环己基-4,4-二甲基-3-羟基-2-（1,2,4-三唑-1-基） - 戊-1-烯-1-酮的（+） - 对映体的制备方法，恩
公开(公告)号：US4789746A
公开(公告)日：1988-12-06
申请号：US835843
申请日：1986-03-03
申请人： Udo Kraatz , Peter Feyen
发明人： Udo Kraatz , Peter Feyen
IPC分类号： C07D249/08 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A process for the preparation of the (+)-antipode of (E)-1-cyclohexyl-4,4-dimethyl-3-hydroxy-2-(1,2,4-tri-azol-1-yl)-pent -1-ene of the formula ##STR1## which comprises reacting the (E)-isomer of 1-cyclohexyl-4,4-dimethyl-2-(1,2,4-triazol-1-yl)-pent-1-en-3-one of the formula ##STR2## with lithium aluminum hydride in the presence of an inert organic diluent and in the presence of a chiral amino alcohol at a temperature between -80.degree. C. and +50.degree. C. The (+)-antipode is produced in high selectivity, using (+)-N-methyl-ephedrine.
摘要翻译：（E）-1-环己基-4,4-二甲基-3-羟基-2-（1,2,4-三唑-1-基） - 酮的（+） - 对映体的制备方法 -1-烯，其包括使1-环己基-4,4-二甲基-2-（1,2,4-三唑-1-基） - 戊-1-烯-1-酮的（E） - 异构体在惰性有机稀释剂存在下，在手性氨基醇存在下，在-80℃至+ 50℃之间的温度下，将式（IMAGE）的3- ） - 使用（+） - N-甲基 - 麻黄碱以高选择性产生 -

2. 发明授权

US5230892A Solid formulations 失效
标题翻译：固体制剂
公开(公告)号：US5230892A
公开(公告)日：1993-07-27
申请号：US911992
申请日：1992-07-10
申请人： Peter Feyen , Uwe Priesnitz , Raphael Wieschollek , Wolfgang Thielert , Stefan Dutzmann , Dieter Feucht , Ulrike Wachendorff-Neumann
发明人： Peter Feyen , Uwe Priesnitz , Raphael Wieschollek , Wolfgang Thielert , Stefan Dutzmann , Dieter Feucht , Ulrike Wachendorff-Neumann
IPC分类号： A01N25/14
CPC分类号： A01N25/14
摘要： New solid formulations ofA) at least one agrochemical active compound,B) at least one additive from the groups mentioned in the description,C) at least one dispersant,D) at least one carrier andE) if appropriate, further active compounds and/or additives,a process for preparing the solid formulations and their use for treating plants.A new device for preparing new granules.
摘要翻译： A）至少一种农药活性化合物的新固体制剂，B）至少一种来自本说明书中所述基团的添加剂，C）至少一种分散剂，D）至少一种载体，E）如果合适的话，还可加入其它活性化合物和 /或添加剂，制备固体制剂的方法及其用于处理植物的用途。一种用于制备新颗粒的新装置。

3. 发明授权

US4327040A Preparation of phosphoric acid propargyl esters 失效
标题翻译：磷酸炔丙酯的制备
公开(公告)号：US4327040A
公开(公告)日：1982-04-27
申请号：US158032
申请日：1980-06-09
申请人： Gunter Arend , Peter Feyen
发明人： Gunter Arend , Peter Feyen
IPC分类号： A01N57/10 , B01J27/00 , C07B61/00 , C07F9/113 , C07F9/14 , C07F9/173
CPC分类号： C07F9/173 , C07F9/113 , C07F9/1403
摘要： A process for the preparation of a phosphoric acid propargyl ester of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is an aryl radical or a C.sub.1-4 -alkyl, C.sub.1-4 -alkenyl or C.sub.1-4 -alkynyl radical, andX, Y and Z each independently is oxygen or sulphur, comprising reacting a phosphoric acid monoester chloride or diester chloride with at least the equivalent amount of propargyl alcohol in a two-phase system in the presence of an inorganic base as an acid-trapping agent, and a catalyst comprising about 0.001 to 100 mol %, relative to the phosphoric acid ester chloride, of a tertiary amine or quaternary ammonium or phosphonium salt with at least 9 C atoms. Advantageously the catalyst is present in about 0.01 to 10 mol % relative to the phosphoric acid ester chloride and is a tertiary amine or quaternary ammonium salt, X, Y and Z are oxygen, R.sup.1 is propargyl and R.sup.2 is C.sub.1-4 -alkyl, the reaction is effected in the presence of methylene chloride, chloroform or toluene as solvent, the base is used in at least the equivalent amount and is selected from the group consisting of alkali metal hydroxides, alkaline earth metal hydroxides, alkali metal carbonates and alkaline earth metal carbonates.
摘要翻译：一种制备下式的磷酸炔丙酯的方法，其中R 1和R 2各自独立地是芳基或C 1-4 - 烷基，C 1-4 - 烯基或C 1-4 - 炔基，X ，Y和Z各自独立地是氧或硫，包括在无机碱作为酸捕获剂的存在下，使磷酸单酯氯化物或二酯氯化物与至少相当量的炔丙醇在两相体系中反应，和相对于磷酸酯氯化物含有至少9个C原子的叔胺或季铵或鏻盐的约0.001至100摩尔％的催化剂。有利地，催化剂相对于磷酸酯氯化物以约0.01至10mol％存在，并且是叔胺或季铵盐，X，Y和Z是氧，R 1是炔丙基，R 2是C 1-4 - 烷基，反应在二氯甲烷，氯仿或甲苯作为溶剂的存在下进行，碱至少使用等量的碱金属氢氧化物，碱土金属氢氧化物，碱金属碳酸盐和碱土金属碳酸盐

4. 发明授权

US4215118A 2-Hetero-acetamido-penicillanates and cephalosporinates 失效
标题翻译： 2-异乙酰氨基 - 青霉烷酸和头孢菌素
公开(公告)号：US4215118A
公开(公告)日：1980-07-29
申请号：US923518
申请日：1978-07-10
申请人： Michael Preiss , Hans-bodo Konig , Karl G. Metzger , Peter Feyen
发明人： Michael Preiss , Hans-bodo Konig , Karl G. Metzger , Peter Feyen
IPC分类号： A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D231/12 , C07D277/20 , C07D277/48 , C07D307/54 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/34 , C07D501/46 , C07D501/57 , A61K31/535 , C07D499/44
CPC分类号： C07D231/12 , C07D277/48 , C07D277/587 , C07D307/54 , C07D499/00
摘要： 2-Hetero-acetamido-penicillanates and cephalosporinates of the formula ##STR1## in which R is hydrogen or lower alkoxy,Z is ##STR2## R.sup.1 and R.sup.2 independently or together are various radicals, A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## n is 1 or 2, X is S,O,SO,SO.sub.2 or --CH.sub.2 --,Y is the balance of a penicillin or cephalosporin moiety, andB is a heterocyclic radical, in the form of the acid, a hydrate thereof, a salt thereof or a salt of the hydrate, exhibit marked anti-bacterial properties rendering them suited for use as antibiotics and animal feed supplements.
摘要翻译：其中R是氢或低级烷氧基的式“IMAGE”的2-异 - 乙酰氨基 - 青霉烷酸酯和头孢烯酸酯，Z独立地或一起是各种基团，A是-CH 2 -CH 2 - ， - CH2-CH2-或 n为1或2，X为S，O，SO，SO2或-CH2-，Y为青霉素或头孢菌素部分的余量，B为杂环基，酸，其水合物，其盐或水合物的盐表现出显着的抗菌性能，使其适合用作抗生素和动物饲料添加剂。

5. 发明授权

US4200576A Beta-lactam antibiotics 失效
标题翻译： β-内酰胺类抗生素
公开(公告)号：US4200576A
公开(公告)日：1980-04-29
申请号：US862466
申请日：1977-12-20
申请人： Peter Feyen , Michael Preiss , Karl G. Metzger
发明人： Peter Feyen , Michael Preiss , Karl G. Metzger
IPC分类号： C07D499/66 , A61K31/415 , A61K31/42 , A61K31/43 , A61K31/435 , A61K31/505 , A61K31/535 , A61K31/545 , A61P31/04 , C07D233/38 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/20 , C07D501/57
CPC分类号： C07D233/38 , C07D499/00 , Y02P20/55
摘要： Antibacterially active and animal feedstuff supplement .beta.-lactam antibiotics of the formula ##STR1## in which R is H or --UR',U is O or S,R' is optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl or cycloalkyl,Z is ##STR2## R.sup.1 and R.sup.2 individually are hydrogen or, individually or together with the carbon atom to which they are bonded, are any of various radicals,A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## B is optionally substituted phenyl or is cyclohexenyl or cyclohexadienyl; X is S, O, SO, SO.sub.2 or --CH.sub.2 --; andY is a group of the formula ##STR4## T is hydrogen, alkyl--CO--O--, pyridinium, aminopyridinium, carbamoyloxy, azido, cyano, hydroxyl or optionally substituted --S--phenyl, or is --S--Het, in whichHet is an optionally substituted heterocyclic 5-membered or 6-membered ring; and whereinE is hydrogen, a radical forming, with the carboxyl group to which it is attached, a carboxy ester group, a cation of a salt, or a protective group,or a hydrate thereof. A process is also given for converting R directly from H to UR' employing a base, a halogenating agent and R'UH .
摘要翻译：抗菌活性和动物饲料补充式为其中R为H或-UR'的式（I）的β-内酰胺抗生素，U为O或S，R'为任选取代的烷基，烯基，炔基，芳烷基，芳基或环烷基，Z是R 1和R 2各自独立地是氢，或者与它们所键合的碳原子单独或一起是各种基团中的任何一个，A是-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或 - B是任选取代的苯基或环己烯基或环己二烯基; X是S，O，SO，SO 2或-CH 2 - ; 并且Y是下式的基团：T是氢，烷基-CO-O-，吡啶鎓，氨基吡啶鎓，氨基甲酰氧基，叠氮基，氰基，羟基或任选取代的-S-苯基，或者是-S-Het，其中 Het是任选取代的杂环5元或6元环; 其中E为氢，与其连接的羧基形成的自由基为羧基酯基，盐的阳离子或保护基或其水合物。还给出了使用碱，卤化剂和R'UH将R直接从H转化为UR'的方法。

6. 发明授权

US4929735A Process for the preparation of oxiranes 失效
标题翻译：环氧乙烷的制备方法
公开(公告)号：US4929735A
公开(公告)日：1990-05-29
申请号：US185211
申请日：1988-04-22
申请人： Wolf Reiser , Peter Feyen
发明人： Wolf Reiser , Peter Feyen
IPC分类号： C07D405/06 , C07D301/02 , C07D303/08 , C07D303/22 , C07D521/00
CPC分类号： C07D303/22 , C07D231/12 , C07D233/56 , C07D249/08 , C07D303/08
摘要： A process for the preparation of an oxirane of the formula ##STR1## in which X is 4-chlorobenzyl, 4-phenylphenoxy or 1H-(1,2,4)-triazolyl,comprising reacting dimethyl sulphate with an excess of dimethyl sulphide thereby to form trimethylsulphonium methyl-sulphate of the formula(CH.sub.3).sub.3 S.sym.CH.sub.3 SO.sub.4 .crclbar.,and without prior isolation reacting the trimethylsulphonium methyl-sulphate with a keytone of the formula ##STR2## in the presence of solid potassium hydroxide or sodium hydroxide in dimethyl sulphide at a temperature between 0.degree. C. and 50.degree. C.
摘要翻译：制备式“IMAGE”的环氧乙烷的方法，其中X是4-氯苄基，4-苯基苯氧基或1H-（1,2,4） - 三唑基，包括使硫酸二甲酯与过量的二甲基硫醚反应，从而形成式（CH 3）3 S（+）CH 3 SO 4（ - ）的三甲基锍甲基硫酸盐，并且不经事先分离，在固体氢氧化钾或氢氧化钠存在下，使甲基硫酸三甲基锍与式二硫化碳在0℃至50℃的温度下进行。

7. 发明授权

US4537730A Preparation of O,S-dimethyl-thiolophosphoric acid amide 失效
标题翻译：制备O，S-二甲基 - 硫代磷酸酰胺
公开(公告)号：US4537730A
公开(公告)日：1985-08-27
申请号：US516167
申请日：1983-07-21
申请人： Peter Feyen , Hermann Seifert , Egon Kohler
发明人： Peter Feyen , Hermann Seifert , Egon Kohler
IPC分类号： C07F9/24
CPC分类号： C07F9/24
摘要： A simplified process for preparing the known insecticide 0,S-dimethylthiolphosphoric acid amide of the formula ##STR1## inexpensively, in high purity and with minimum waste water and gas which would have to be specially treated to avoid environmental pollution, comprises(a) contacting 0,0 dimethyl-thiophosphoric acid amide of the formula ##STR2## in which Me is sodium or potassium, separating the aqueous phase,(b) optionally adding an organic solvent to the aqueous phase, and reacting the mass with methyl bromide or methyl chloride thereby to form the 0,S-dimethyl-thiolphosphoric acid amide, and either(c) extracting the amide with a sparingly water-miscible solvent thereby to dissolve the amide, or(d) concentrating the reaction mixture from the methylation step (b), by distillation, until the alkali metal halide formed has separated out, and filtering off the alkali metal halide.
摘要翻译：制备低成本的已知杀虫剂0，S-二甲基硫代磷酸酰胺的简便方法是以高纯度和最少的废水和气体制备，该方法必须经过特殊处理以避免环境污染，其包括（a）接触其中Me是钠或钾的0,0二甲基 - 硫代磷酸酰胺，其中Me是钠或钾，分离水相，（b）任选地向水相中加入有机溶剂，并使该物质与甲基溴或甲基氯从而形成0S-二甲基 - 硫醇磷酸酰胺，和（c）用少量与水混溶的溶剂萃取酰胺，从而溶解酰胺，或（d）从甲基化步骤（b）浓缩反应混合物，通过蒸馏，直到形成的碱金属卤化物分离出来，并过滤掉碱金属卤化物。

8. 发明授权

US4501897A Process for the preparation of E-isomers of 1-cyclohexyl-2-(1,2,4-triazol-1-yl)-1-penten-3-one derivatives 失效
标题翻译： 1-环己基-2-（1,2,4-三唑-1-基）-1-戊烯-3-酮衍生物的E-异构体的制备方法
公开(公告)号：US4501897A
公开(公告)日：1985-02-26
申请号：US523537
申请日：1983-08-16
申请人： Wolf Reiser , Hans-Ludwig Elbe , Peter Feyen
发明人： Wolf Reiser , Hans-Ludwig Elbe , Peter Feyen
IPC分类号： C07D209/08 , C07D249/08 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A process for the preparation of E-isomers of 1-cyclohexyl-2-(1,2,4-triazol-1-yl)-1-penten-3-one derivatives of the formula ##STR1## in which X and Y independently of one another represent hydrogen or halogen by contacting isomers of 1-cyclohexyl-2-(1,2,4-triazol-1-yl)-1-penten-3-one derivatives of the formula ##STR2## in which X and Y have the previously indicated meaning with at least one secondary amine, if desired in the presence of water and/or in the presence of a water immiscible solvent.
摘要翻译：制备式（I）的1-环己基-2-（1,2,4-三唑-1-基）-1-戊烯-3-酮衍生物的E-异构体的方法，其中X 和Y彼此独立地表示氢或卤素，通过使式（VI）的1-环己基-2-（1,2,4-三唑-1-基）-1-戊烯-3-酮衍生物的异构体），其中如果需要，在水的存在下和/或在与水不混溶的溶剂的存在下，X和Y具有至少一个仲胺的前述含义。

9. 发明授权

US4338434A 2-Hetero-acetamido-cephalosporinates 失效
标题翻译： 2-异乙酰氨基头孢菌素
公开(公告)号：US4338434A
公开(公告)日：1982-07-06
申请号：US45474
申请日：1979-06-04
申请人： Michael Preiss , Hans-Bodo Konig , Karl G. Metzger , Peter Feyen
发明人： Michael Preiss , Hans-Bodo Konig , Karl G. Metzger , Peter Feyen
IPC分类号： A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D231/12 , C07D277/20 , C07D277/48 , C07D307/54 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/34 , C07D501/46 , C07D501/57
CPC分类号： C07D231/12 , C07D277/48 , C07D277/587 , C07D307/54 , C07D499/00
摘要： 2-Hetero-acetamido-penicillanates and cephalosporinates of the formula ##STR1## in which R is hydrogen or lower alkoxy,Z is ##STR2## R.sup.1 and R .sup.2 independently or together are various radicals, A is --CH.sub.2 --CH.sub.2 --,--CH.sub.2 --CH.sub.2 --CH.sub.2 -- or ##STR3## n is 1 or 2, X is S,O,SO,SO.sub.2 or --CH.sub.2 --,Y is the balance of a penicillin or cephalosporin moiety, andB is a heterocyclic radical, in the form of the acid, a hydrate thereof, a salt thereof or a salt of the hydrate, exhibit marked anti-bacterial properties rendering them suited for use as antibiotics and animal feed supplements.
摘要翻译：其中R为氢或低级烷氧基的式“IMAGE”的2-异 - 乙酰氨基 - 青霉烷酸和头孢菌素，Z为独立地或一起为不同的基团，A为-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - 或 n为1或2，X为S，O，SO，SO 2或-CH 2 - ，Y为青霉素或头孢菌素部分的余量，B为杂环基，的酸，其水合物，其盐或水合物的盐表现出显着的抗菌性质，使其适合用作抗生素和动物饲料添加剂。

10. 发明授权

US4218451A Penicillins and their use 失效
标题翻译：青霉素及其用途
公开(公告)号：US4218451A
公开(公告)日：1980-08-19
申请号：US920505
申请日：1978-06-29
申请人： Peter Feyen , Hans-Bodo Konig , Karl G. Metzger
发明人： Peter Feyen , Hans-Bodo Konig , Karl G. Metzger
IPC分类号： C07D499/66 , A61K31/43 , A61K31/495 , A61P31/04 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/64 , C07D499/68
CPC分类号： C07D499/00
摘要： New penicillins of the formula ##STR1## in which ##STR2## E is oxygen or sulphur, and R.sub.1 and R.sub.2 are hydrogen or various organic radicals with certain provisos,or salts thereof, are antibacterially ative and useful as antibiotics in pharmacy, as animal feed supplements for promoting growth, and as preservatives.
摘要翻译：其中 E是氧或硫，R1和R2是氢或具有某些条件的各种有机基团或其盐的新型青霉素具有抗菌活性并且可用作抗生素在药房，作为促进生长的动物饲料补充剂和防腐剂。

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