公开(公告)号：US20060004198A1

公开(公告)日：2006-01-05

申请号：US10511968

申请日：2003-04-16

申请人： Jan Vermehren ,  Mark Ford ,  Gunter Schlegel ,  Iswald Ort ,  Boerries Kuebel

发明人： Jan Vermehren ,  Mark Ford ,  Gunter Schlegel ,  Iswald Ort ,  Boerries Kuebel

IPC分类号： C07D43/02

CPC分类号： C07D251/42 ,  C07C303/22 ,  C07C309/89

摘要： The invention relates to a preparation process for the compound (I) or a salt thereof where Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) monoesterifying a compound (II) where Hal=a halogen atom, giving (III), b) either b1) ammonolysing and phosgenating this compound to give (V) or b2) converting this compound with cyanate into (V) and c) converting the resulting compound (V) with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) into the compound (I) or a salt thereof. Some compounds (II) and some intermediates (VIII), stabilized with N-heteroaromatic compounds, of the compounds (V) are novel. The compounds (II) can be obtained from the corresponding sulfobenzoic acids by reaction with acid halides of sulfur or phosphorus in nonpolar organic solvents.

摘要翻译： 本发明涉及其中Q，X *，Y，Z，R，R 1，R 2和R 2的化合物（I）或其盐的制备方法 其中包括a）其中Hal =卤素原子的化合物（II）的单酯化，得到（III），b）b1）氨解和光气化该化合物，得到（ V）或b2）将该化合物与氰酸酯转化为（V），和c）将所得化合物（V）与氨基杂环H 2 N-Het（Het =如（I）中的杂环））转化成 化合物（I）或其盐。 化合物（V）的一些化合物（II）和一些由N-杂芳族化合物稳定的中间体（VIII））是新颖的。 化合物（II）可以通过在非极性有机溶剂中与硫或磷的酰卤反应从相应的磺基苯甲酸获得。

公开(公告)号：US06500952B1

公开(公告)日：2002-12-31

申请号：US09664201

申请日：2000-09-18

申请人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

发明人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

IPC分类号： C07D23942

CPC分类号： C07D521/00 ,  A01N47/36 ,  H01R33/06 ,  Y02A40/143

摘要： The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A=H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.

摘要翻译： 本发明涉及化合物（Ⅰ）的制备，其中A = H或酰基，R 1，R 21，R 3，R 4，n，X，Y和Z如权利要求1中所定义，通过卤化和重排化合物 任选的盐），得到化合物（III）a）（III）至（IV）的氨解，硝基的还原和与式Ar-OCO-N（M）-Het的氨基甲酸酯（盐）（VI）的反应， 其中Ar =苯基，M = H或阳离子和Het =来自式（I）的杂环，得到（III）至（IV）化合物（I）（A = H），orb）氨解，与氨基甲酸酯 （VI）和还原所得化合物（VII）在NO 2基团上得到化合物（I）（A = H），orc）（III）与式HNR3-Het的氰酸酯和胺（VIII）的反应，还原 所得到的化合物（Ⅶ）在NO2基团上得到化合物（I）（A = H），任选的酰化如果A不为H.式（I）（A = H），（III） （IV），（V），（VI）（M =阳离子）和（VII）是新颖的。

公开(公告)号：US5424480A

公开(公告)日：1995-06-13

申请号：US162858

申请日：1993-12-06

申请人： Jan Vermehren ,  Gunther Heubach ,  Peter Braun ,  Burkhard Sachse

发明人： Jan Vermehren ,  Gunther Heubach ,  Peter Braun ,  Burkhard Sachse

IPC分类号： A01N37/38 ,  A01N41/10 ,  A01N55/00 ,  C07C259/06 ,  C07C317/22 ,  C07F7/08 ,  C07F7/10 ,  C09D7/12 ,  C07C239/10

CPC分类号： C07C259/06 ,  A01N37/38 ,  C07F7/0818

摘要： The invention relates to novel N-alkoxycinnamamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 are alkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxyalkenyl, alkoxyalkynyl, trialkylsilylalkynyl or arylalkyl, aryl optionally being substituted by alkyl, alkoxy, haloalkyl, haloalkoxy, alkoxycarbonyl, halogen, cyano, nitro, alkylsulfonyl, phenyl and/or phenoxy, to processes for their preparation, to fungicidal compositions containing them, and to their use as fungicides.

摘要翻译： 本发明涉及式I（I）的新型N-烷氧基肉桂酰胺，其中R 1和R 2为烷基，烯基，炔基，烷氧基烷基，烷氧基烯基，烷氧基炔基，三烷基甲硅烷基炔基或芳烷基，任选被烷基，烷氧基， ，卤代烷氧基，烷氧基羰基，卤素，氰基，硝基，烷基磺酰基，苯基和/或苯氧基，其制备方法，含有它们的杀真菌组合物及其作为杀真菌剂的用途。

公开(公告)号：US07057043B2

公开(公告)日：2006-06-06

申请号：US10936180

申请日：2004-09-08

申请人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

发明人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

IPC分类号： C07D239/02

CPC分类号： C07D521/00 ,  A01N47/36 ,  H01R33/06 ,  Y02A40/143

摘要： The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) R*═OH, R**═NR1R2  (II) R*═NR1R2, R**═Cl  (III) R*═NR1R2, R**═NH2  (IV) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (V) of the formula HNR3−Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A=H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.

公开(公告)号：US5258520A

公开(公告)日：1993-11-02

申请号：US003648

申请日：1993-01-13

申请人： Wolfgang Giencke ,  Jan Vermehren

发明人： Wolfgang Giencke ,  Jan Vermehren

IPC分类号： C07D213/84 ,  C07D215/48 ,  C07D217/26 ,  C07D221/04 ,  C07D213/57

CPC分类号： C07D213/84 ,  C07D215/48 ,  C07D217/26 ,  C07D221/04

摘要： Compounds of the formula I ##STR1## in which R.sup.1 is H, alkyl, alkenyl, alkynyl, haloalkyl, alkoxycarbonyl, alkoxyalkyl, phenyl, benzyl or phenoxyalkyl, it being possible for the three latter radicals to be substituted in the phenyl moiety;R.sup.2 is H, alkyl, alkenyl, alkynyl, haloalkyl or alkoxycarbonyl;R.sup.3 is H, alkyl, alkenyl, alkynyl, haloalkyl, alkoxycarbonyl, phenyl, phenoxy, benzyl, it being possible for the three latter radicals to be substituted, or alkoxy; andR.sup.4 is H, alkyl, alkenyl, alkynyl, haloalkyl or alkoxycarbonyl;orR.sup.1 together with R.sup.2 is a saturated chain, and the remaining radicals are as defined above;orR.sup.1 together with R.sup.2 is a chain of the formula --CH.dbd.CH--CH.dbd.CH--, which may be substituted, and the remaining radicals are as defined above;orR.sup.3 together with R.sup.4 is a chain of the formula --CH.dbd.CH--CH.dbd.CH--, which may be substituted, and the remaining radicals are as defined above;are valuable intermediates in the preparation of pharmaceuticals and crop protection agents.The process according to the invention yields compounds of the formula I by reacting a substituted 1-alkoxypyridinium salt of the formula II, ##STR2## in which R.sup.1 to R.sup.4 have the same meaning as in formula I andR.sup.5 is alkyl, alkenyl, alkynyl, benzyl or trialkylsilyl andX is a leaving group;together with a cyanide of the formula IIIM(CN).sub.m (III)in whichM is alkali metal, alkaline earth metal or copper andm is 1 or 2,in a polar, aprotic solvent or mixture of solvents.

摘要翻译： 其中R 1为H，烷基，烯基，炔基，卤代烷基，烷氧基羰基，烷氧基烷基，苯基，苄基或苯氧基烷基的式I化合物，其后三个基团可以在苯基部分被取代; R2是H，烷基，烯基，炔基，卤代烷基或烷氧基羰基; R3是H，烷基，烯基，炔基，卤代烷基，烷氧基羰基，苯基，苯氧基，苄基，三个后面的基团可以被取代，或烷氧基; R4是H，烷基，烯基，炔基，卤代烷基或烷氧基羰基; 或R 1与R 2一起为饱和链，其余基团如上所定义; 或R 1与R 2一起是式-CH = CH-CH = CH-的链，其可以被取代，其余基团如上所定义; 或R 3与R 4一起是式-CH = CH-CH = CH-的链，其可以被取代，其余基团如上所定义; 是制备药物和作物保护剂的有价值的中间体。 根据本发明的方法通过使式II的取代的1-烷氧基吡啶鎓盐，其中R 1至R 4具有与式I中相同的含义，并且R 5为烷基，链烯基，炔基 苄基或三烷基甲硅烷基，X是离去基团; 连同其中M为碱金属，碱土金属或铜，m为1或2的式III M（CN）m（III）的氰化物在极性，非质子溶剂或溶剂混合物中。

公开(公告)号：US06790955B2

公开(公告)日：2004-09-14

申请号：US10288052

申请日：2002-11-05

申请人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

发明人： Gerhard Schnabel ,  Jan Vermehren ,  Lothar Willms

IPC分类号： C07D27300

CPC分类号： C07D521/00 ,  A01N47/36 ,  H01R33/06 ,  Y02A40/143

摘要： The invention relates to the preparation of compounds (I) in which A═H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M═H or cation and Het=heterocycle from formula (I), to give compounds (I) (A═H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A═H), or c) reaction of (III) with cyanates and amines (VII) of the formula HNR3-Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A═H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A═H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.

摘要翻译： 本发明涉及其中A = H或酰基和R 1，R 2，R 3，R 3，n，X，Y和Z如权利要求1中所定义的化合物（I）的制备， 化合物（II）（任选盐）的卤化和重排以得到化合物（III）a）（III）至（IV）的氨解，还原硝基并与式Ar-的氨基甲酸酯（盐）（Ⅵ） 其中Ar =苯基，M = H或阳离子和Het =来自式（I）的杂环，得到化合物（I）（A = H），orb）氨解（III）至（III） IV），与氨基甲酸酯（盐）（VI）的反应和NO 2基团上得到的化合物（VII）的还原，得到化合物（I）（A = H），orc）（III）与氰酸酯和胺的反应（VII） 的式（HNR 3）-Het，并且在NO 2基上还原所得化合物（Ⅶ），得到化合物（I）（A = H），并且如果A不为H，则为任意的酰化。式 I）（A = H），（III），（IV），（V），（VI）（M =阳离子）和（VII）

公开(公告)号：US5550237A

公开(公告)日：1996-08-27

申请号：US415696

申请日：1995-04-03

申请人： Jan Vermehren

发明人： Jan Vermehren

IPC分类号： B01J23/44 ,  B01J31/22 ,  C07B61/00 ,  C07C303/22 ,  C07C309/58 ,  C07C327/16 ,  C07D295/192

CPC分类号： C07C303/22

摘要： Compounds (I) in which Ar is (substituted) arylene and Nuc is the radical of a nucleophile Nuc-H and which are valuable intermediates for pharmaceuticals, crop protection products and colorantsHO.sub.3 S--Ar--CO--NUC (I)can be prepared according to the invention by reacting an internal diazonium salt of the formula (II).sup..crclbar. O.sub.3 S--Ar--N.sub.2.sup..sym.with CO in the presence of a metal catalyst of group VIII of the Periodic System or Cu and Nuc-H or a salt thereof.

摘要翻译： 其中Ar是（取代的）亚芳基和Nuc的化合物（I）是亲核试剂Nuc-H的基团，它们是药物，作物保护产品和着色剂有价值的中间体。可以根据 本发明通过使式（II）（ - ）O 3 S-Ar-N 2（+）的内部重氮盐与CO在周期系统的Ⅷ族金属催化剂或Cu和Nuc-H或其盐 其中。

公开(公告)号：US5164393A

公开(公告)日：1992-11-17

申请号：US776811

申请日：1991-10-15

申请人： Jan Vermehren ,  Wolfgang Giencke ,  Peter Braun ,  Burkhard Sachse

发明人： Jan Vermehren ,  Wolfgang Giencke ,  Peter Braun ,  Burkhard Sachse

IPC分类号： A01N43/54 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D401/04 ,  A01N43/54 ,  C07D403/04

摘要： Pyrimidine derivatives of the formula I ##STR1## in which the variables are herein below described in the specification. R.sup.3, R.sup.4 and R.sup.5 optionally together with the radical R.sup.3 are a component of a maximally unsaturated .lambda.-membered ring where .lambda. is 3 to 8, two radicals R.sup.6 to R.sup.9 together may form a component of an unsaturated or saturated m-membered ring where m is 5 or 6,k is 0, 1 or 2,n is 1 or 2and the addition salts thereof, their preparation, compositions containing them, and their use in the control of harmful fungi.

摘要翻译： 式I的嘧啶衍生物（I）其中变量在本说明书中在下文中描述。 R3，R4和R5任选地与基团R 3一起是λ为3至8的最大不饱和的λ-元环的组分，两个基团R6至R9一起可以形成不饱和或饱和的五元环的组分，其中m 为5或6，k为0,1或2，n为1或2及其加成盐，其制备方法，含有它们的组合物及其在控制有害真菌中的用途。

公开(公告)号：US07781611B2

公开(公告)日：2010-08-24

申请号：US09732006

申请日：2000-12-07

申请人： Mark James Ford ,  Jan Vermehren

发明人： Mark James Ford ,  Jan Vermehren

IPC分类号： C07C309/27 ,  C07C309/29

CPC分类号： C07C303/38 ,  C07C303/22 ,  C07C309/59 ,  C07C311/65 ,  C07D239/52 ,  C07D327/04 ,  C07C311/16 ,  C07C309/89

摘要： The present invention relates to a compound of the formula (I) wherein R1 is an unsubstituted or substituted hydrocarbon radical having a total of 1 to 10 carbon atoms, preferably 1 to 6 carbon atoms, R2 is an unsubstituted or substituted hydrocarbon radical having a total of 1 to 10 carbon atoms, preferably 1 to 6 carbon atoms, or the group NR1R2 is a heterocyclic ring having 3 to 8 ring atoms which is unsubstituted or substituted and contains the nitrogen atom of the group NR1R2 as ring heteroatom and may also contain one or two further ring heteroatoms from the group consisting of N, O and S, and Q is H or a cation. The compounds of the present invention can advantageously be used for the preparation of sulfonylureas and their precursors such as sulfochlorides or sulfonamides.

摘要翻译： 本发明涉及式（I）化合物，其中R 1是总共具有1至10个碳原子，优选1至6个碳原子的未取代或取代的烃基，R 2是未取代或取代的烃基，其具有总计 1〜10个碳原子，优选1〜6个碳原子，或者NR1R2是具有3〜8个环原子的杂环，其未被取代或取代，并且含有NR1R2基团的氮原子作为环杂原子，并且还可以含有一个 或另外两个来自N，O和S的环杂原子，Q是H或阳离子。 本发明的化合物可以有利地用于制备磺酰脲类及其前体如磺酰氯或磺酰胺。

公开(公告)号：US07026477B1

公开(公告)日：2006-04-11

申请号：US10089288

申请日：2000-09-28

申请人： Jan Vermehren ,  Ernst Schmidt ,  Mark James Ford ,  Richard W. G. Foster ,  Ian A. Bourne

发明人： Jan Vermehren ,  Ernst Schmidt ,  Mark James Ford ,  Richard W. G. Foster ,  Ian A. Bourne

IPC分类号： C07D251/18

CPC分类号： C07D251/42

摘要： The invention relates to a preparation process for a compound (I) or a salt thereof, in which Q, X*, Y, Z, R, R1, R2 and R3 are as defined in claim 1, which comprises a) ammonolyzing a comp. (II) in which Hal=halogen atom to give (III), pref. (a1) carrying out the reaction in an organic solvent mixture (org. solv. mixture) comprising (1) opt. halogenated aromatic hydrocarbons and (2) polar aprotic solvents, in a weight ratio of solv. (1): solv. (2) of 20:1 to 1:1, (b) phosgenating the comp. (III) with phenylsulfonyl isocyanate of the formula (IV), pref. (b1) in the case X*=halogen, carrying out the reaction with phosgene in an org. solv. in the presence of isocyanates R′-NCO as catalyst, where R′=(subst.) hydrocarbon, with or without addition of an amine base, (c) reacting the resulting compound (IV) in org. solv. with the aminoheterocycle H2N-Het (Het=heterocycle as in (I)) to give the comp. (I) or a salt thereof, pref. (c1) carrying out the reaction in a solv. mixture of opt. halogenated arom. hydrocarbon having a b.p. of more than 110° C. and a polar aprotic solv., where at least one of the preferred partial steps (a1) to (c1) is carried out in the process.

摘要翻译： 本发明涉及一种化合物（I）或其盐的制备方法，其中Q，X *，Y，Z，R，R 1，R 2， R 3和R 3如权利要求1所定义，其包括：a） （II），其中Hal =卤素原子以得到（III），优选的。 （a1）在包含（1）选择的有机溶剂混合物（有机溶剂混合物）中进行反应。 卤代芳烃和（2）极性非质子溶剂，重量比为溶剂。 （1）：solv。 （2）为20：1至1：1，（b）使化合物光气化。 （III）与式（IV）的苯基磺酰基异氰酸酯反应， （b1）在X * =卤素的情况下，在组织中进行与光气的反应。 解决方案 在异氰酸酯R'-NCO作为催化剂的存在下，其中R'=（取代）烃，具有或不添加胺碱，（c）使所得化合物（IV）在有机溶剂中反应。 解决方案 与氨基杂环H 2 N-Het（Het =如（I）中的杂环））反应，得到化合物。 （I）化合物或其盐。 （c1）在溶剂中进行反应。 混合选择 卤化芳香。 b。 超过110℃的极性非质子溶剂，其中优选的部分步骤（a1）至（c1）中的至少一个在该过程中进行。