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1. 发明授权

US06365739B1 Process for the preparation of 4,6-disubstituted 2-isocyanatopyrimidines and their use as intermediates for active compound syntheses 失效
标题翻译：用于制备4,6-二取代的2-异氰酸基嘧啶的方法及其作为活性化合物合成的中间体的用途
公开(公告)号：US06365739B1
公开(公告)日：2002-04-02
申请号：US09358297
申请日：1999-07-21
申请人： Mark James Ford , Stephen Lachhein
发明人： Mark James Ford , Stephen Lachhein
IPC分类号： C07D23942
CPC分类号： C07D239/545
摘要： Isocyanates of the formula (I) in which X and Y are defined as in formula (I) of claim 1 can be prepared by reacting a compound of the formula (II) or its salts in which X and Y are defined as in formula (I), with 1 to 6 mol of phosgene per mole of compound of the formula (II), in the presence of 2 to 3.5 molar equivalents of a base per mole of compound of the formula (II) and in the presence of an aprotic organic solvent at a reaction temperature in the range from −30 to +60° C. to give the compound of the formula (I). The compounds (I) can be converted by reaction with nucleophiles to give addition products, such as carbamates, ureas and sulfonylureas and corresponding products, e.g. herbicidal sulfonylureas.
摘要翻译：其中X和Y如权利要求1的式（I）中定义的式（I）的异氰酸酯可以通过使式（II）化合物或其盐，其中X和Y如式），在每摩尔式（II）化合物的2至3.5摩尔当量的碱存在下，并且在非质子有机物存在下，每摩尔式（II）的化合物具有1至6摩尔的光气溶剂，反应温度为-30〜+ 60℃，得到式（I）化合物。化合物（I）可以通过与亲核试剂反应而转化，得到加成产物，例如氨基甲酸酯，脲和磺酰脲类及相应的产品，例如。除草磺酰脲类。

2. 发明授权

US4824949A Process for the preparation of pyrimidines 失效
标题翻译：制备嘧啶的方法
公开(公告)号：US4824949A
公开(公告)日：1989-04-25
申请号：US132483
申请日：1987-12-14
申请人： Stephen Lachhein , Lothar Willms
发明人： Stephen Lachhein , Lothar Willms
IPC分类号： C07D239/52 , C07D239/56 , C07D239/58 , C07D239/47
CPC分类号： C07D239/56 , C07D239/52 , C07D239/58
摘要： Process for the preparation of pyrimidines Pyrimidines of the formula I ##STR1## in which X and Y, independently of one another, denote oxygen or sulfur, R.sup.1 and R.sup.2, independently of one another, denote (C.sub.1 --C.sub.4) alkyl, (C.sub.1 --C.sub.4 -alkoxy)-C.sub.1 --C.sub.2 -alkyl or halo-C.sub.1 --C.sub.4 -alkyl, and R.sup.3 denotes C.sub.1 --C.sub.4 -alkyl, phenyl or phenoxy which may both be substituted by one, two or three radicals from the series comprising halogen, C.sub.1 --C.sub.4 -alkoxy and C.sub.1 --C.sub.4 -alkyl radicals, halo-C.sub.1 --C.sub.4 -alkyl or C.sub.1 --C.sub.4 -alkoxy, are obtained in a process in which propanediimidates of the formula II ##STR2## or salt thereof, are reacted with N-cyanoamides of the formula NC--NR.sup.4 --CO--R.sup.3 in which R.sup.4 denotes hydrogen or a cation, in an inert solvent. The compounds of the formula I are suitable as intermediates for the preparation of herbicidal sulfonylureas.
摘要翻译：制备嘧啶的方法式I的嘧啶其中X和Y彼此独立地表示氧或硫，R 1和R 2彼此独立地表示（C 1 -C 4）烷基，（C 1 -C 4）烷基 -C 1-4 - 烷氧基）-C 1 -C 2 - 烷基或卤代C 1 -C 4 - 烷基，R 3表示可以被一个，两个或三个基团取代的C 1 -C 4烷基，苯基或苯氧基，所述基团包括卤素， C 1 -C 4 - 烷氧基和C 1 -C 4 - 烷基，卤代-C 1 -C 4 - 烷基或C 1 -C 4 - 烷氧基是在下式的过程中获得的：其中式II II或其盐的丙二酰亚胺酯或其盐与在惰性溶剂中，其中R 4表示氢或阳离子的式NC-NR4-CO-R3的N-氰酰胺。式I的化合物适用作制备除草磺酰脲类的中间体。

3. 发明授权

US5013444A Process for separating off enol ethers from reaction mixtures containing alcohols 失效
标题翻译：从含有醇的反应混合物中分离出烯醇醚的方法
公开(公告)号：US5013444A
公开(公告)日：1991-05-07
申请号：US576934
申请日：1990-08-29
申请人： Hilmar Mildenberger , Stephen Lachhein , Siegbert Rittner , Heribert Tetzlaff
发明人： Hilmar Mildenberger , Stephen Lachhein , Siegbert Rittner , Heribert Tetzlaff
IPC分类号： C07C29/86 , C07C31/02 , C07C31/04 , C07C41/38 , C07C43/15
CPC分类号： C07C41/38
摘要： The invention relates to a gentle process for the separation of enol ethers from mixtures containing water-soluble alcohols by extraction, wherein an aqueous solution of a base is used as the extraction agent in a phase ratio of the amounts of the aqueous phase: enol ether/alcohol mixture of at least 0.5:1 and the extraction is carried out in several stages or continuously with a theoretical number of stages of at least two. The process is particularly suitable for separating off enol ethers which readily decompose during distillation.
摘要翻译：本发明涉及一种用于通过萃取从烯醇醚与含有水溶性醇的混合物中分离出温和的方法，其中将碱的水溶液用作提取剂，其水相量为：烯醇醚 /醇混合物至少为0.5：1，萃取过程分几个阶段或连续进行，理论数量为至少两个阶段。该方法特别适用于分离在蒸馏过程中容易分解的烯醇醚。

4. 发明授权

US4831138A Process for the preparation of aminopyrimidines 失效
标题翻译：氨基嘧啶的制备方法
公开(公告)号：US4831138A
公开(公告)日：1989-05-16
申请号：US132484
申请日：1987-12-14
申请人： Stephen Lachhein
发明人： Stephen Lachhein
IPC分类号： C07D239/54 , C07D239/52 , C07D239/56 , C07D239/58
CPC分类号： C07D239/56 , C07D239/52 , C07D239/58
摘要： Process for the preparation of aminopyrimidinesPyrimidines of the formula I ##STR1## in which X and Y denote oxygen or sulfur and R.sup.1 and R.sup.2 denote C.sub.1 -C.sub.4 -alkyl, (C.sub.1 -C.sub.4 -alkoxy)-C.sub.1 -C.sub.2 -alkyl or halo-C.sub.1 -C.sub.4 -alkyl, are obtained through reaction of propanediimidates of the formula II ##STR2## or salts thereof with cyanurates of the formula R.sup.3 --O--CN in which R.sup.3 denotes C.sub.1 -C.sub.4 -alkyl, phenyl, phenyl which is substituted by 1, 2 or 3 radicals from the series comprising halogen, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -alkyl radicals, .alpha.- or .beta.-naphthyl or halo-C.sub.1 -C.sub.4 -alkyl, in an organic solvent which is inert under the reaction conditions. The one-step process permits efficient preparation of the compounds of the formula I, which can be used as intermediates for the preparation of herbicidal sulfonylureas.
摘要翻译：制备氨基嘧啶的方法式I的嘧啶其中X和Y表示氧或硫，R 1和R 2表示C 1 -C 4 - 烷基，（C 1 -C 4 - 烷氧基）-C 1 -C 2 - 烷基或卤代 C 1 -C 4 - 烷基是通过式II II的丙二酰亚胺酯或其盐与式R3-O-CN的氰尿酸酯反应得到的，其中R 3表示C 1 -C 4 - 烷基，苯基，被取代的苯基包含卤素，C 1 -C 4 - 烷氧基和C 1 -C 4 - 烷基，α或β-萘基或卤代-C 1 -C 4 - 烷基的一系列基团在有机溶剂中反应，该有机溶剂在反应条件。一步法可有效制备式I化合物，其可用作制备除草磺酰脲的中间体。

5. 发明授权

US4599207A Process for the preparation of phosphorus-containing cyanohydrin derivatives 失效
标题翻译：含磷氰醇衍生物的制备方法
公开(公告)号：US4599207A
公开(公告)日：1986-07-08
申请号：US614846
申请日：1984-05-29
申请人： Stephen Lachhein , Hilmar Mildenberger
发明人： Stephen Lachhein , Hilmar Mildenberger
IPC分类号： C07F9/32
CPC分类号： C07F9/3211
摘要： The invention relates to a new process for the preparation of compounds of the formula (I) ##STR1## in which R.sub.1 denotes alkyl and R.sub.2 denotes H, acetyl or propionyl, by addition of compounds of the formula II ##STR2## onto compounds of the formula III, using radical-formers, the radical-formers being used being compounds of the general formula IV ##STR3## in which R.sub.3 denotes alkyl or phenyl and R.sub.4 denotes alkyl, the reaction being carried out at temperatures in the range from 50.degree. to 100.degree. C., and, for the preparation of compounds of the formula I where R.sub.2 is H, then splitting off the radical R.sub.2.sup.'. Using this process, the compounds of the formula I are obtained in high yield and particular purity.
摘要翻译：本发明涉及一种制备式（I）化合物的新方法，其中R 1表示烷基，R 2表示H，乙酰基或丙酰基，通过将式II的化合物加到使用自由基形成剂的式III化合物使用的自由基形成剂是通式IV（IV）的化合物，其中R 3表示烷基或苯基，R 4表示烷基，反应在在50℃至100℃的范围内，并且为了制备其中R 2为H的式I化合物，然后将R2'分解。使用该方法，以高产率和特别纯度获得式I化合物。

6. 发明授权

US5157121A Process for the preparation of N-alkylsulfonylaminosulfonylureas 失效
标题翻译：制备N-烷基磺酰氨基脲的方法
公开(公告)号：US5157121A
公开(公告)日：1992-10-20
申请号：US731460
申请日：1991-07-17
申请人： Stephen Lachhein , Lothar Willms
发明人： Stephen Lachhein , Lothar Willms
IPC分类号： A01N43/54 , A01N47/36 , C07D239/42 , C07D239/47 , C07D239/48 , C07D239/52 , C07D521/00
CPC分类号： C07D521/00
摘要： Known herbicides of the formula (I) ##STR1## in which R.sup.1 is alkyl, alkenyl or alkynyl, which are optionally substituted by halogen, alkoxy or alkoxycarbonyl,R.sup.2 is H, alkyl, alkenyl, alkynyl or cycloalkyl,R.sup.3 and R.sup.4 are H or alkyl,R.sup.5 and R.sup.6 are H, alkyl or alkoxy, each of which can be substituted by halogen, alkoxy or alkylthio, or are halogen, alkylthio, alkylamino or dialkylamino,or, if R.sup.2 or R.sup.3 is H, their salts with bases, can be obtained when compounds of the formula IIR.sup.1 --SO.sub.2 --NR.sup.2 --SO.sub.2 --NR.sup.3 --CO--OR.sup.7(II)in whichR.sup.1, R.sup.2 and R.sup.3 are as defined above,are reacted with compounds of the formula III ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are as defined above andR.sup.7 is alkyl, haloalkyl or optionally substituted phenyl,in an inert organic solvent, to give the compounds of the formula I.
摘要翻译：式（I）的已知除草剂其中R 1为任选被卤素，烷氧基或烷氧基羰基取代的烷基，烯基或炔基，R 2为H，烷基，烯基，炔基或环烷基，R 3和R 4 卤素，烷硫基，烷基氨基或二烷基氨基，或者如果R2或R3是H，则它们的盐与当其中R 1，R 2和R 3如上定义的式IIR 1 -SO 2 -NR 2 -SO 2 -NR 3 -CO-OR 7（II）的化合物与式III化合物反应时，可以得到碱。（III）其中R4，R5和R6如上定义，R7是烷基，卤代烷基或任选取代的苯基，在惰性有机溶剂中，得到式I化合物。

7. 发明授权

US5124470A Process for the preparation of arylalkylmethylsilanes 失效
标题翻译：制备芳基甲基硅氧烷的方法
公开(公告)号：US5124470A
公开(公告)日：1992-06-23
申请号：US732792
申请日：1991-07-19
申请人： Stephen Lachhein
发明人： Stephen Lachhein
IPC分类号： C07F7/08 , C07F7/12
CPC分类号： C07F7/12 , C07F7/0896
摘要： The present invention relates to a process for the preparation of arylalkylmethylsilanes of the formula I ##STR1## where X is CH.dbd.CH, N.dbd.CH, CH.dbd.N or S,R.sup.1 and R.sup.2 independently of one another are H, halogen, (C.sub.1 to C.sub.4)alkyl, (C.sub.1 to C.sub.4)alkoxy, (C.sub.1 to C.sub.4)alkylthio, (C.sub.1 to C.sub.4)haloalkyl, (C.sub.1 to C.sub.4)haloalkoxy or (C.sub.1 to C.sub.4)haloalkylthio,R.sup.3 is (C.sub.1 to C.sub.6)alkyl andm and n are 0, 1 or 2,which comprises reacting dichloromethylsilane II ##STR2## first with an arylmagnesium halide of the formula III ##STR3## where R.sup.1, R.sup.2, m, n and X are as defined in Formula I and Hal is halogen, at temperatures of from -78.degree. to 0.degree. C., and subsequently with an alkylmagnesium halide of the formula IVR.sup.3 --Mg Hal (IV),where R.sup.3 is as defined in formula I and Hal is halogen, if appropriate in the presence of a solvent.
摘要翻译：本发明涉及制备式I（I）的芳基烷基甲基硅烷的方法，其中X为CH = CH，N = CH，CH = N或S，R 1和R 2彼此独立地为H，卤素，（C1至C4）烷基，（C1至C4）烷氧基，（C1至C4）烷硫基，（C1至C4）卤代烷基，（C1至C4）卤代烷氧基或（C1至C4）卤代烷硫基，R3为（C1至C6）烷基和m和n为0,1或2，其包括首先使二氯甲基硅烷II（II）与式III的芳基卤化镁（III）反应，其中R 1，R 2，m，n和X为在式I中定义，Hal为卤素，在-78℃至0℃的温度下，随后与式IV的R3-Mg Hal（IV）的烷基镁卤化物反应，其中R 3如式I所定义，Hal为如果合适的话，在溶剂的存在下是卤素。

8. 发明授权

US5070201A Process for the preparation of aminopyrimidines 失效
标题翻译：氨基嘧啶的制备方法
公开(公告)号：US5070201A
公开(公告)日：1991-12-03
申请号：US601224
申请日：1990-10-22
申请人： Stephen Lachhein , Lothar Willms
发明人： Stephen Lachhein , Lothar Willms
IPC分类号： C01C3/16 , C07D239/52 , C07D239/56 , C07D239/58
CPC分类号： C07D239/56 , C07D239/52 , C07D239/58
摘要： Aminopyrimidines of the formula (I) ##STR1## in which X and Y are in each case oxygen or sulfur andR.sup.1, R.sup.2 are independently of one another (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy-(C.sub.1 -C.sub.2)alkyl or halo(C.sub.1 -C.sub.4)alkyl,are intermediates for the preparation of herbicides from the sulfonylurea group. According to the invention, compounds of the formula I can be prepared in a one-step process without pH control, which comprises the reaction of a propanediimidate of the formulaR.sup.1 X--C(.dbd.NH)--CH.sub.2 --C(.dbd.NH)--YR.sup.2or its salt with an alkali metal or alkaline earth metal salt of the cyanamide, in which a solution of the compounds in an alcohol of the formula R.sup.4 --OH, in which R.sup.4 is (C.sub.1 -C.sub.6)alkyl, or, simultaneously, separate solutions of the compounds in each case in an alcohol R.sup.4 --OH are added to an inert organic solvent which is higher-boiling in comparison to the alcohol at temperatures above 100.degree. C. with simultaneous removal of the alcohol by distillation.
摘要翻译：其中X和Y各自为氧或硫，R1，R2彼此独立地为（C1-C4）烷基，（C1-C4）烷氧基 - （C1-C2）烷基））烷基或卤代（C 1 -C 4）烷基是用于从磺酰脲基团制备除草剂的中间体。根据本发明，式I化合物可以在没有pH控制的一步法中制备，其包括式R1X-C（= NH）-CH2-C（= NH）-YR2的丙二酰亚胺酸酯或其盐与氨基氰的碱金属或碱土金属盐，其中化合物在式R 4 -OH的醇中的溶液，其中R 4是（C 1 -C 6）烷基，或同时分离溶液在各种情况下，在醇R 4 -OH中的化合物加入惰性有机溶剂中，与醇在高于100℃的温度下相比，沸点更高，同时通过蒸馏除去醇。

9. 发明授权

US5294741A Continuous process for the preparation of sulfonylisocyanates 失效
标题翻译：连续制备磺酰基异氰酸酯的方法
公开(公告)号：US5294741A
公开(公告)日：1994-03-15
申请号：US839790
申请日：1992-02-21
申请人： Gunter Schlegel , Stephen Lachhein , Harald Berger
发明人： Gunter Schlegel , Stephen Lachhein , Harald Berger
IPC分类号： C07C303/40 , C07C311/65
CPC分类号： C07C311/65
摘要： The invention relates to an improved process for the preparation of a compound of the formula R.sup.1 -X-SO.sub.2 -NCO in whichX is O or NR.sup.2,R.sup.1 is alkylsulfonyl or phenyl which is optionally substituted by Hal, alkyl and/or alkoxy, andR.sup.2 is alkyl, by reactingR.sup.1 XH with ClSO.sub.2 NCO to give the compound R.sup.1 XCONHSO.sub.2 Cl followed by a rearrangement reaction, which comprises carrying out the process continuously in the presence or absence of an inert solvent.
摘要翻译：本发明涉及制备其中X为O或NR2的R1-X-SO2-NCO化合物，R1为烷基磺酰基或任选被Hal，烷基和/或烷氧基取代的苯基的改进方法，以及 R 2是烷基，通过使R1XH与ClSO2NCO反应，得到化合物R1XCONHSO2Cl，随后进行重排反应，其包括在惰性溶剂存在或不存在下连续进行该方法。

10. 发明授权

US5159086A Process for the preparation of pyrazolecarboxylic acid derivatives 失效
标题翻译：制备吡唑并吡啶酸衍生物的方法
公开(公告)号：US5159086A
公开(公告)日：1992-10-27
申请号：US643449
申请日：1991-01-18
申请人： Stephen Lachhein
发明人： Stephen Lachhein
IPC分类号： C07D231/14
CPC分类号： C07D231/14
摘要： Process for the preparation of pyrazolecarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 independently of one another is haloalkyl or halogen,R.sup.2 is alkyl or alkynyl,R.sup.3 is an alkali metal or alkaline earth metal, hydrogen, alkyl or alkoxyalkyl andn=1 or 2, by reaction of a compound of the formula II ##STR2## in which Z is chlorine or bromine, with an enol ether of the formula III ##STR3## in which R.sup.5 is alkyl, to give a compound of the formula IV ##STR4## and its subsequent aromatization to give the compound I, wherein the reaction of the compound II with the compound III to give the compound IV is carried out in a 2-phase system (aqueous/organic) in the presence of an inorganic base at temperatures of 40.degree.-100.degree. C. and at pH values of 7-10 and then the compound IV formed is aromatized, without prior isolation, under acidic conditions in a 2-phase system (aqueous/organic) to give the compound of the formula I.
摘要翻译：制备式I的吡唑羧酸衍生物的方法其中R 1彼此独立地是卤代烷基或卤素，R 2是烷基或炔基，R 3是碱金属或碱土金属，氢，烷基或烷氧基烷基和n = 1或2，其中Z为氯或溴的式II化合物（II）与式III的烯醇醚（III）反应，其中R 5为烷基得到式IV的化合物（IV）及其随后的芳构化，得到化合物I，其中化合物II与化合物III反应得到化合物IV的反应在2-相体系中进行（水/有机）在无水碱存在下，在40-100℃的温度和pH值为7-10的条件下，然后将所形成的化合物IV芳构化，在酸性条件下，在2- 相系统（水/有机），得到式I的化合物。

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