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81. 发明授权

US4224226A Process for the production of N-substituted .alpha.-ketocarboxylic acid amides 失效
标题翻译：制备N-取代的α-酮羧酸酰胺的方法
公开(公告)号：US4224226A
公开(公告)日：1980-09-23
申请号：US926322
申请日：1978-07-20
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 , C07C102/08
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 groups 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）式“IMAGE”（ IV）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。

82. 发明授权

US4222956A Process for the production of cyanocarboxylic acids 失效
标题翻译：制备氰基羧酸的方法
公开(公告)号：US4222956A
公开(公告)日：1980-09-16
申请号：US12133
申请日：1979-02-14
申请人： Axel Kleemann , Peter Schalke , Detlef Arnoldi
发明人： Axel Kleemann , Peter Schalke , Detlef Arnoldi
IPC分类号： C07C255/19 , C07C20060101 , C07C67/00 , C07C253/00 , C07C120/00 , C07C121/407
CPC分类号： C07C255/00
摘要： Cyanocarboxylic acids are prepared by reacting halocarboxylic acids with cyanohydrins, preferably at a pH of 9 to 11.
摘要翻译：氰基羧酸通过卤代羧酸与氰醇反应制备，优选在9至11的pH下进行。

83. 发明授权

US4175088A Process for the production of [1,1-dithienyl-(3)-1-hydroxypropyl-(3)]-[1-phenyl-1-hydroxypropyl-(2)]-a mine and [1,1-dithienyl-(3)-propen-(1)-yl-(3)]-[1-phenylpropyl-(2)]-amine 失效
标题翻译：制备[1,1-二噻吩基 - （3）-1-羟基丙基 - （3）] - [1-苯基-1-羟丙基 - （2）] - 胺和[1,1-二噻吩基 - （3 ） - 丙烯 - （1） - 基 - （3）] - [1-苯基丙基 - （2）] - 胺
公开(公告)号：US4175088A
公开(公告)日：1979-11-20
申请号：US867294
申请日：1978-01-05
申请人： Axel Kleemann , Reinhold Kiel , Ingomar Nubert
发明人： Axel Kleemann , Reinhold Kiel , Ingomar Nubert
IPC分类号： C07D333/14 , A61K31/382 , C07D333/16 , C07D333/20
CPC分类号： C07D333/16 , C07D333/20
摘要： [1,1-dithien-(3)-yl-1-hydroxy-(3)-propyl]-[1-phenyl-1-hydroxy-(2)-propyl]-amine is prepared by condensing thien-(3)-yl lithium with a .beta.-halogen propionic acid alkyl ester of the formula ##STR1## where R is a lower alkyl group and Hal is chlorine, bromine or iodine, in an inert medium at a temperature below -50.degree. C. to form a compound of the formula ##STR2## which is then reacted with 2-amino-1-hydroxy-1-phenylpropane in an inert medium in the presence of a basic compound. The product cn be converted to [1,1-dithien-(3)-yl-(1)-propen-(3)-yl]-[1-phenyl-(2)-propyl]-amine by dehydration.
摘要翻译：通过将噻吩（3） - （3） - （1） - 羟基 - （3） - 丙基] - [1-苯基-1-羟基 - （2）） - 基锂与式（II）的β-卤代丙酸烷基酯反应，其中R是低级烷基，Hal是氯，溴或碘，在惰性介质中，温度低于-50℃ 形成式（III）的化合物，然后在碱性化合物的存在下，在惰性介质中与2-氨基-1-羟基-1-苯基丙烷反应。通过脱水将产物转化为[1,1-二噻吩 - （3） - 基 - （1） - 丙烯 - （3） - 基] - [1-苯基 - （2） - 丙基] - 胺。

84. 发明授权

US5707933A Herbicidal pyrazolyloxy-picolinamides 失效
标题翻译：除草吡唑氧基 - 吡啶酰胺
公开(公告)号：US5707933A
公开(公告)日：1998-01-13
申请号：US463279
申请日：1995-06-05
申请人： Axel Kleemann , Robert John Griffith Searle
发明人： Axel Kleemann , Robert John Griffith Searle
IPC分类号： A01N43/56 , A01P13/00 , C07D401/12 , C07D401/02
CPC分类号： C07D401/12 , A01N43/56
摘要： Herbicidal picolinamide derivatives are provided having the formula I ##STR1## which Z represents an oxygen or sulphur atom, R.sup.1 and R.sup.2 each independently represents a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, alkaryl, hydroxy, alkoxy, alkenyloxy, alkynyloxy, alkylcarbonyl, amino, mono- or di-alkylamino, alkoxycarbonylamino, arylamino, arylalkylamino or dialkylcarbamoyl group, or together represent an alkylene chain which is optionally interrupted by an oxygen, or sulphur atom or by a group --NR-- in which R represents a hydrogen atom or an alkyl group, R.sup.3 independently represents a halogen atom or an alkyl or haloalkyl group, R.sup.4, R.sup.5 and R.sup.6 each independently represents a hydrogen or halogen atom, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, alkaryl, alkoxy, amino, mono- or di-alkylamino, alkoxycarbonylamino, arylamino, dialkylcarbamoyl, acyl or acylamido group or a cyano group, with the proviso that R.sup.5 and R.sup.6 do not represent an acyl, acylamido or cyano group, and n represents 0, 1, 2 or 3.
摘要翻译：提供除草的吡啶酰胺衍生物，其具有式I（I），其中Z表示氧或硫原子，R1和R2各自独立地表示氢原子或任选取代的烷基，烯基，炔基，环烷基，环烷基烷基，芳基，芳烷基，烷芳基，羟基，烷氧基，烯氧基，炔氧基，烷基羰基，氨基，单 - 或二 - 烷基氨基，烷氧基羰基氨基，芳基氨基，芳基烷基氨基或二烷基氨基甲酰基，或一起表示任选被氧或硫原子中断的亚烷基链，基团-NR-，其中R表示氢原子或烷基，R3独立地表示卤素原子或烷基或卤代烷基，R4，R5和R6各自独立地表示氢或卤素原子，任选取代的烷基，烯基，炔基，环烷基，环烷基烷基，芳基，芳烷基，烷芳基，烷氧基，氨基，单 - 或二 - 烷基氨基，烷氧基羰基氨基，芳基氨基，二烷基氨基甲酰基，酰基或酰基酰氨基或ac yano基团，条件是R 5和R 6不表示酰基，酰氨基或氰基，n表示0,1,2或3。

85. 发明授权

US4966732A Process for the production of 1,2-dithiolan-3-pentanoic acid (thioctic acid) and 8-hydrocarbylthio-6-oxooctanoic acid 失效
标题翻译：生产1,2-二硫戊环-3-戊酸（硫辛酸）和8-烃基硫代-6-氧代辛酸的方法
公开(公告)号：US4966732A
公开(公告)日：1990-10-30
申请号：US73584
申请日：1987-07-15
申请人： Guenes Giray , Klaus Huthmacher , Axel Kleemann , Thomas Lied
发明人： Guenes Giray , Klaus Huthmacher , Axel Kleemann , Thomas Lied
IPC分类号： C07C323/52 , A61K31/385 , A61P1/16 , A61P25/00 , C07C67/00 , C07C313/00 , C07C319/06 , C07C319/14 , C07C319/20 , C07C323/22 , C07C327/22 , C07D339/04
CPC分类号： C07D339/04 , C07C323/00
摘要： 1,2-Dithiolane-3-pentanoic acid (D,L-thioctic acid) of the formula ##STR1## is prepared by a process comprising (a) reacting a 2-(3-alkylthiopropionyl)-cyclopentanone-1 of the formula ##STR2## where R is a C.sub.1 -C.sub.4 alkyl, phenyl or benzyl in aqueous alkaline solution at a temperature of about 20.degree. C. to about 90.degree. C. to form the corresponding carboxylic acid of formula VI ##STR3## (b) reacting the compound of formula VI with an alkyl mercaptan at a temperature between -20.degree. C. and 0.degree. C. to form the corresponding thioketal of formula VII ##STR4## (c) reacting the compound of formula VII with sodium in liquid ammonia at temperature temperture between -60.degree. C. and -10.degree. C. to form the 6,8-dimercaptooctanic acid of formual VIII ##STR5## (d) reacting the 6,8-dimercaptooctanoic acid of formula VIII in alkaline solution with an iron (III) salt and oxygen to form the 1,2-dithiolane-3-pentanoic acid of formula IX, or in place of steps (a) through (c) reacting an acid of formula XII ##STR6## where R.sub.1 and R.sub.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl or benzyl, with the proviso that both R.sub.1 and R.sub.2 cannot be benzyl, with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the corresponding 6,8-dimercaptooctanoic acid of formula VIII. The compounds of formulae VI, VII, XII are new.

86. 发明授权

US4824987A Method of preparing m-trifluoromethylphenyl acetonitrile 失效
标题翻译：制备三氟甲基苯基乙腈的方法
公开(公告)号：US4824987A
公开(公告)日：1989-04-25
申请号：US197343
申请日：1988-05-23
申请人： Axel Kleemann , Herbert Klenk , Klaus Huthmacher , Dieter Most
发明人： Axel Kleemann , Herbert Klenk , Klaus Huthmacher , Dieter Most
IPC分类号： C07C253/04 , C07C255/32 , C07C255/33 , C07C255/35 , C07C120/00
CPC分类号： C07C255/00
摘要： A method of preparing m-trifluoromethylphenyl acetonitrile of the formula ##STR1## in which m-trifluoromethyl toluene is reacted with cyanogen chloride in the gas phase at 600.degree. to 750.degree. C.
摘要翻译：制备式“IMAGE”的间三氟甲基苯基乙腈的方法，其中间 - 三氟甲基甲苯与氯化氰在气相中在600至750℃下反应。

87. 发明授权

US4716242A Salts of oxazaphosphorine derivatives 失效
标题翻译：恶唑烷衍生物的盐
公开(公告)号：US4716242A
公开(公告)日：1987-12-29
申请号：US704465
申请日：1985-02-22
申请人： Jurgen Engel , Axel Kleemann , Ulf Niemeyer , Peter Hilgard , Joerg Pohl
发明人： Jurgen Engel , Axel Kleemann , Ulf Niemeyer , Peter Hilgard , Joerg Pohl
IPC分类号： C07F9/24 , A61K31/675 , A61P35/00 , A61P35/02 , C07F9/22 , C07F9/6584 , C07F9/40
CPC分类号： C07F9/65846
摘要： There are provided new antitumor salts of oxazaphosphorine derivatives of the formula ##STR1## where R.sub.1, R.sub.2, and R.sub.3 are the same or different and represent hydrogen, methyl, ethyl, 2-chloroethyl, or 2-methanesulfonyloxyethyl and wherein at least two of these residues are 2-chloroethyl and/or 2-methanesulfonyl-oxyethyl and A is the group --S--alk--SO.sub.3 H or --N(OH)--CONH--alk--CO.sub.2 H and alk represents a C.sub.2 -C.sub.6 -alkylene residue optionally containing a mercapto group, whereby alk also can be --CH.sub.2 -- in case there is a carboxy group attached to the alk group, with homocysteinethiolactone or .alpha.-amino-.epsilon.-caprolactam or a basic compound of the formula: ##STR2## wherein R.sub.4 is a hydroxy group, an amino group or a C.sub.1 -C.sub.6 -alkoxy group, R.sub.5 is hydrogen or a difluoromethyl group, R.sub.6 is hydrogen, an indolyl-(3)-methyl residue, imidazolyl-(4)-methyl residue, a C.sub.1 -C.sub.10 -alkyl group or a C.sub.1 -C.sub.10 -alkyl group which is substituted by a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a mercapto group, a C.sub.1 -C.sub.6 -alkylmercapto group, a phenyl group, a hydroxy phenyl group, an amino-C.sub.1 -C.sub.6 -alkylmercapto group, an amino-C.sub.1 -C.sub.6 -alkoxy group, an amino group, an aminocarbonyl group, a ureido group (H.sub.2 NCONH--), a guanidino group or a C.sub.1 -C.sub.6 -alkoxycarbonyl group, or wherein R.sub.6 together with the structured portion >CR.sub.5 (NR.sub.7 R.sub.8) forms the proline residue, the 4-hydroxy-proline residue or the 2-oxo-3-amino-3-difluoromethyl-piperidine and the residues R.sub.7 and R.sub.8 represent hydrogen or C.sub.1 -C.sub.6 -alkyl residues.
摘要翻译：提供了新的式（ⅩⅧ）的恶唑烷磷衍生物的抗肿瘤盐，其中R 1，R 2和R 3相同或不同，代表氢，甲基，乙基，2-氯乙基或2-甲磺酰氧基乙基，其中这些残基是2-氯乙基和/或2-甲磺酰氧基乙基，A是-S-烷基-SO 3 H或-N（OH）-CONH-烷基-CO 2 H，烷基代表任选含有巯基的C 2 -C 6亚烷基其中烷基也可以是-CH 2 - ，如果存在与烷基连接的羧基，具有同半胱氨酸硫内酯或α-氨基 - ε-己内酰胺或下式的碱性化合物：其中R 4是羟基基团，氨基或C1-C6-烷氧基，R5是氢或二氟甲基，R6是氢，吲哚基 - （3） - 甲基残基，咪唑基 - （4） - 甲基残基，C1-C10- 烷基或被羟基，C1-C6-烷氧基，巯基，C1-C6烷基巯基取代的C1-C10-烷基基团，苯基，羟基苯基，氨基-C 1 -C 6烷基巯基，氨基-C 1 -C 6烷氧基，氨基，氨基羰基，脲基（H 2 NCONH-），胍基或C 1 -C 6烷氧基羰基，或其中R 6与结构部分> CR 5（NR 7 R 8）一起形成脯氨酸残基，4-羟基 - 脯氨酸残基或2-氧代-3-氨基-3-二氟甲基 - 哌啶和残基R7和R8表示氢或C1-C6烷基残基。

88. 发明授权

US4705867A Process for the production of 1,2-dithiolan-3-pentanoic acid (thioctic acid) and intermediate compounds therefor 失效
标题翻译：生产1,2-二硫戊环-3-戊酸（硫辛酸）及其中间体化合物的方法
公开(公告)号：US4705867A
公开(公告)日：1987-11-10
申请号：US848212
申请日：1986-04-04
申请人： Guenes Giray , Klaus Huthmacher , Axel Kleemann , Thomas Lied
发明人： Guenes Giray , Klaus Huthmacher , Axel Kleemann , Thomas Lied
IPC分类号： C07C323/52 , A61K31/385 , A61P1/16 , A61P25/00 , C07C67/00 , C07C313/00 , C07C319/06 , C07C319/14 , C07C319/20 , C07C323/22 , C07C327/22 , C07D339/04
CPC分类号： C07D339/04 , C07C323/00
摘要： 1,2-Dithiolane-3-pentanoic acid (D,L-thioctic acid) of the formula ##STR1## is prepared by a process comprising (a) reacting a 2-(3-alkylthiopropionyl)-cyclopentanone-1 of the formula ##STR2## where R is a C.sub.1 -C.sub.4 alkyl, phenyl or benzyl in aqueous alkaline solution at a temperature of about 20.degree. C. to about 90.degree. C. to form the corresponding carboxylic acid of formula VI ##STR3## (b) reacting the compound of formula VI with an alkyl mercaptan at a temperature between -20.degree. C. and 0.degree. C. to form the corresponding thioketal of formula VII ##STR4## (c) reacting the compound of formula VII with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the 6,8-dimercaptooctanoic acid of formula VIII ##STR5## (d) reacting the 6,8-dimercaptooctanoic acid of formula VIII in alkaline solution with an iron (III) salt and oxygen to form the 1,2-dithiolane-3-pentanoic acid of formula IX, or in place of steps (a) through (c) reacting an acid of formula XII ##STR6## where R.sub.1 and R.sub.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl or benzyl, with the proviso that both R.sub.1 and R.sub.2 cannot be benzyl, with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the corresponding 6,8-dimercaptooctanoic acid of formula VIII. The compounds of formulae VI, VII, XII are new.
摘要翻译：式（IX）的1,2-二硫戊环-3-戊酸（D，L-硫辛酸）是通过以下方法制备的，该方法包括：（a）使式（I）的2-（3-烷硫基丙酰基） - 环戊酮-1 V，其中R是在约20℃至约90℃的温度下在碱性水溶液中的C 1 -C 4烷基，苯基或苄基，以形成相应的式VI的羧酸）使式Ⅵ化合物与烷基硫醇在-20℃至0℃之间的温度下反应，形成相应的式Ⅶ的缩酮醛Ⅶ（c）使式Ⅶ化合物与液体中的钠反应在-60℃至-10℃的温度下加入氨以形成式VIII的6,8-二巯基辛酸VIII（d）使式VIII的6,8-二巯基辛酸在碱性溶液中与铁（III）盐和氧气以形成式IX的1,2-二硫戊环-3-戊酸，或代替步骤（a）至（c）使式XI的酸其中R 1和R 2是氢，C 1 -C 4 - 烷基，苯基或苄基，条件是R 1和R 2不能是苄基，钠在液氨中在-60℃和-60℃之间， 10℃，形成相应的式VIII的6,8-二巯基辛酸。式VI，VII，XII的化合物是新的。

89. 发明授权

US4628126A Process for the production of dihydroxybenzenes 失效
标题翻译：二羟基苯的制备方法
公开(公告)号：US4628126A
公开(公告)日：1986-12-09
申请号：US588847
申请日：1984-03-12
申请人： Karlheinz Drauz , Axel Kleemann
发明人： Karlheinz Drauz , Axel Kleemann
IPC分类号： B01J27/00 , B01J27/02 , C07B61/00 , C07C27/00 , C07C37/60 , C07C39/08 , C07C67/00 , C07C37/00
CPC分类号： C07C37/60 , Y02P20/582
摘要： The nuclear hydroxylation of phenol with organic solutions of hydrogen peroxide in the presence of a catalyst is carried out in improved manner by employing both (1) a special, practically water free solution of hydrogen peroxide in an organic solvent which does not form an azeotrope with water or whose highest azeotrope with water, boil near or above the boiling point of hydrogen peroxide, and (2) employing as a catalyst XO.sub.2 where X is sulfur, selenium, or tellurium. Besides increasing the yield and the ability to carry out the reaction in a simpler manner when selenium dioxide is employed as a catalyst, there can also be controlled the ortho-para ratio, respectively, the ortho-ortho ratio of the product.
摘要翻译：在催化剂存在下，用过氧化氢的有机溶液对苯酚进行核羟基化处理是通过使用（1）特殊的实际上无水的过氧化氢在不与共沸物形成共沸物的有机溶剂中，水或其与水的共沸物最高，沸点接近或高于过氧化氢的沸点，和（2）使用X为硫，硒或碲的催化剂XO2。当使用二氧化硒作为催化剂时，除了增加产率和以更简单的方式进行反应的能力之外，还可以分别控制产物的邻位比。

90. 发明授权

US4551562A Process for the production of dihydroxybenzenes 失效
公开(公告)号：US4551562A
公开(公告)日：1985-11-05
申请号：US588999
申请日：1984-03-13
申请人： Karlheinz Drauz , Axel Kleemann
发明人： Karlheinz Drauz , Axel Kleemann
IPC分类号： B01J27/00 , B01J27/02 , C07B61/00 , C07C27/00 , C07C37/60 , C07C39/08 , C07C67/00 , C07C41/26
CPC分类号： C07C37/60 , Y02P20/582
摘要： The nuclear hydroxylation of phenol with organic solutions of hydrogen peroxide in the presence of a catalyst is carried out in improved manner by employing both (1) a special, practically water free solution of hydrogen peroxide in an organic solvent which does not form an azeotrope with water or whose highest azeotrope with water, boil near or above the boiling point of hydrogen peroxide, and (2) employing as a catalyst XO.sub.2 where X is sulfur, selenium, or tellurium. Besides increasing the yield and the ability to carry out the reaction in a simpler manner when selenium dioxide is employed as a catalyst, there can also be controlled the ortho-para ratio, respectively, the ortho-ortho ratio of the product.

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