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1. 发明授权

US4808572A .alpha.-Hydroxy thioethers 失效
标题翻译： α-羟基硫醚
公开(公告)号：US4808572A
公开(公告)日：1989-02-28
申请号：US936671
申请日：1986-12-01
申请人： Andreas Beck , Werner Breitenstein , Andreas von Sprecher , Robert W. Lang , Konrad Oertle
发明人： Andreas Beck , Werner Breitenstein , Andreas von Sprecher , Robert W. Lang , Konrad Oertle
IPC分类号： A61K31/16 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/23 , A61K38/00 , A61K45/00 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C67/00 , C07C313/00 , C07C321/18 , C07C323/00 , C07C323/52 , C07C323/58 , C07C323/59 , C07C323/60 , C07K1/113 , C07K5/02 , C07K5/06 , C07C149/243
CPC分类号： C07K5/0606 , A61K31/19 , A61K31/215 , C07C323/00 , A61K38/00
摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.1-7 -alkoxy or an optionally substituted amino group, and--X-- represents a single bond, a methylene group of an optionally N-acylated primary aminomethylene group,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
摘要翻译：式（I）的新型不对称硫醚，其中通式具有以下含义：a为1至7的整数，R 4表示氢或C 1-7 - 烷酰基，R 1表示C 1-3 - 烷基，可以在末端碳原子上被游离或酰化的羟基，原子数至多为17的卤素原子或甲氧基取代，或表示C1-3-全氟烷基，R2表示任选不饱和的脂肪族基，其具有 5至15个碳原子，A代表乙烯，或者，如果R1代表卤代基，和/或B代表亚苯基或亚乙基，则单键或亚乙烯基，B代表单键，亚乙炔基或亚苯基，R3代表羟基，C1-7 - 烷氧基或任选取代的氨基，-X-表示单键，任选N-酰化的伯氨基亚甲基的亚甲基，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除平滑肌的收缩b 由白细胞三烯生成，因此适用于治疗过敏性疾病，特别是哮喘病症。

2. 发明授权

US4785004A Aromatic thioethers 失效
标题翻译：芳香硫醚
公开(公告)号：US4785004A
公开(公告)日：1988-11-15
申请号：US941676
申请日：1986-12-15
申请人： Andreas Von Sprecher , Werner Breitenstein , Andreas Beck , Robert W. Lang , Konrad Oertle
发明人： Andreas Von Sprecher , Werner Breitenstein , Andreas Beck , Robert W. Lang , Konrad Oertle
IPC分类号： C07D215/54 , C07D311/24 , C07C149/40 , A61K31/235
CPC分类号： C07D311/24 , C07D215/54
摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
摘要翻译：式（I）的新颖的不对称硫醚，其中通式符号具有以下含义：R 0表示氢或C 1-7 - 烷酰基，R 1表示可以被一个或多个具有原子数最多为17，R 2表示具有5至15个碳原子的脂族基团，A表示乙烯，单键或亚乙烯基，B1表示C1-7 - 亚烷基或亚苯基，B2表示单键，乙烯或亚苯基，M表示部分结构式（M）的芳族基团，其中符号具有以下含义：R 3表示氢或C 1-4 - 烷基，X表示NH，O，S或如果R 4表示氢，则单键，R4和R5之一表示氢，另一个表示-CO-R6基团，或R4和R5一起代表基团-CO-C（R6）= C（R7）-OR-CO-C（ R7）= C（R6） - 或R4R5与X一起代表基团-N = C（R8）-C（R6）= CH-，其中R6表示 - （CH2）b-COOR3（其中b = 0至2）R7表示氢或C1-4烷基，R8表示氢，甲基，乙氧基或卤素，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于治疗过敏，特别是哮喘，病情。

3. 发明授权

US5149717A Alkanophenones useful for treating allergies 失效
标题翻译：用于治疗过敏的苯胺酮
公开(公告)号：US5149717A
公开(公告)日：1992-09-22
申请号：US795227
申请日：1991-11-15
申请人： Andreas von Sprecher , Andreas Beck , Bruno Schaub , Robert W. Lang
发明人： Andreas von Sprecher , Andreas Beck , Bruno Schaub , Robert W. Lang
IPC分类号： C07D311/24 , C07D405/04
CPC分类号： C07D405/04 , C07D311/24
摘要： Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.
摘要翻译：其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌，低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用作为药物中的抗过敏活性成分。

4. 发明授权

US4826965A Metal complexes containing optically active sugar ligands, a process for their preparation and their use as chiral reactants for synthesis of alcohols and amines 失效
标题翻译：含有光学活性糖配体的金属络合物，其制备方法及其作为用于合成醇和胺的手性反应物的用途
公开(公告)号：US4826965A
公开(公告)日：1989-05-02
申请号：US76250
申请日：1987-07-21
申请人： Martin Riediker , Robert W. Lang , Rudolf Duthaler , Peter Herold , Konrad Oertle , Guido Bold
发明人： Martin Riediker , Robert W. Lang , Rudolf Duthaler , Peter Herold , Konrad Oertle , Guido Bold
IPC分类号： C07H15/04 , C07C29/40 , C07C227/32 , C07D319/16 , C07F7/18 , C07H23/00 , C07F7/28
CPC分类号： C07H23/00 , C07C227/32 , C07C29/40 , C07D319/16 , C07F7/1852 , C07F7/1896 , C07B2200/07 , C07B2200/09 , C07C2103/24 , C07C2103/26
摘要： Compounds of the forulae I and Ia ##STR1## in which R.sup.1 is a group which can be transferred to carbonyl or imine compounds, for example alkyl, allyl, vinyl or the radical of an enol or enamine, R.sup.2 is, for example, cyclopentadienyl, R.sup.3 is the radical of an optically active sugar or sugar derivative, Me is Ti, Zr or Hf, x is 0, 1 or 2 and y is 0, 1, 2 or 3, M.sym. is Li.sym., Na.sym., K.sym., MgY.sym., ZnY.sym., CdY.sym., HgY, CuY.sym. or quaternary ammonium, Y being halogen, are suitable for use as chiral reactants for compounds containing aldehyde, keto and/or N-substituted imine groups.
摘要翻译：其中R1是可以转移到羰基或亚胺化合物的基团，例如烷基，烯丙基，乙烯基或烯醇的基团，或者其中R 1是可以转移到羰基或亚胺化合物的基团，烯胺，R2是例如环戊二烯基，R3是光学活性糖或糖衍生物的基团，Me是Ti，Zr或Hf，x是0,1或2，y是0,1,2或3，M （+）是Y为卤素的Li（+），Na（+），K（+），MgY（+），ZnY（+），CdY（+），HgY，CuY（+）或季铵用作用于含有醛，酮和/或N-取代的亚胺基团的化合物的手性反应物。

5. 发明授权

US4914196A Complexes containing optically active sugar ligands, a process for their preparation and their use 失效
标题翻译：含有光学活性糖配体的配合物，其制备方法及其应用
公开(公告)号：US4914196A
公开(公告)日：1990-04-03
申请号：US316127
申请日：1989-02-27
申请人： Martin Riediker , Robert W. Lang , Rudolf Duthaler , Peter Herold , Konrad Oertle , Guido Bold
发明人： Martin Riediker , Robert W. Lang , Rudolf Duthaler , Peter Herold , Konrad Oertle , Guido Bold
IPC分类号： C07H15/04 , C07C29/40 , C07C227/32 , C07D319/16 , C07F7/18 , C07H23/00
CPC分类号： C07H23/00 , C07C227/32 , C07C29/40 , C07D319/16 , C07F7/1852 , C07F7/1896 , C07B2200/07 , C07B2200/09 , C07C2103/24 , C07C2103/26
摘要： Compounds of the formulae I and Ia ##STR1## in which R.sup.1 is a group which can be transferred to carbonyl or imine compounds, for example alkyl, allyl, vinyl or the radical of an enol or enamine, R.sup.2 is, for example, cyclopentadienyl, R.sup.3 is the radical of an optically active sugar or sugar derivative, Me is Ti, Zr or Hf, x is 0, 1 or 2 and y is 0, 1, 2 or 3, M.sup..sym. is Li.sup..sym., Na.sup..sym., K.sup..sym., MgY.sup..sym., ZnY.sup..sym., CdY.sup..sym., HgY, CuY.sup..sym. or quaternary ammonium, Y being halogen, are suitable for use as chiral reactants for compounds containing aldehyde, keto and/or N-substituted imine groups.

6. 发明授权

US5032606A Novel fluorinated resorcinol ethers and their use as anti-allergics and anti-inflammatories 失效
标题翻译：新型氟化间苯二酚醚及其用作抗过敏和抗炎药
公开(公告)号：US5032606A
公开(公告)日：1991-07-16
申请号：US529690
申请日：1990-05-23
申请人： Andreas Beck , Alfred Sallmann , Robert W. Lang , Paul Wenk
发明人： Andreas Beck , Alfred Sallmann , Robert W. Lang , Paul Wenk
IPC分类号： C07C39/24 , C07C43/225 , C07C43/23 , C07C45/46 , C07C45/71 , C07C49/825 , C07C49/84 , C07C205/37 , C07D257/04
CPC分类号： C07D257/04 , C07C205/37 , C07C39/24 , C07C39/245 , C07C43/225 , C07C43/23 , C07C45/46 , C07C45/71 , C07C49/825 , C07C49/84
摘要： 4-Acylresorcinol ethers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties.

7. 发明授权

US4820726A Oxaloamino substituted fluorinated resorcinol ethers and anti-allergic and anti-inflammatory use thereof 失效
标题翻译：草酰胺取代的氟代间苯二酚醚及其抗过敏和抗炎用途
公开(公告)号：US4820726A
公开(公告)日：1989-04-11
申请号：US3156
申请日：1987-01-14
申请人： Andreas Beck , Alfred Sallmann , Robert W. Lang , Paul Wenk
发明人： Andreas Beck , Alfred Sallmann , Robert W. Lang , Paul Wenk
IPC分类号： C07C39/24 , C07C43/225 , C07C43/23 , C07C45/46 , C07C45/71 , C07C49/825 , C07C49/84 , C07C205/37 , C07D257/04 , C07C103/14 , A61K31/165
CPC分类号： C07D257/04 , C07C205/37 , C07C39/24 , C07C39/245 , C07C43/225 , C07C43/23 , C07C45/46 , C07C45/71 , C07C49/825 , C07C49/84
摘要： 4-Acylresorcinol esthers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties. They are prepared, for example, by reacting compounds of the formulae ##STR2## in which one of the radicals X.sub.5 and X.sub.6 is hydroxyl which is free or in salt form and the other is an alkoxy radical substituted by reactive esterified hydroxy or epoxy. The invention also relates to intermediates of the formula ##STR3## in which R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen and R.sub.11 is hydrogen or a group of the formula R.sub.1 --C(--O)--, in which R.sub.1 is lower alkyl, and their salts.
摘要翻译：其中R 1是低级烷基，R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素的式（Ⅰ）的4-酰基间苯二酚衍生物，alk是不间断或中断的亚烷基或羟基亚烷基氧，基团R4，R5和R7之一是式-NH-C（= O）-R8的基团，与此不同的基团R 4或R 5是基团R 9和与此不同的基团R 7，基团R 10，R 6为氢，低级烷基，三氟甲基，卤素，羧基，其游离，酯化或酰胺化，氰基或低级烷酰基，R8为羧基，其为游离的，酯化的或酰胺化的或5-四唑基，R 9为氢，低级烷基，低级烷氧基，卤素或三氟甲基，R 10是氢，低级烷基，低级烷氧基，卤素，三氟甲基，氰基或羧基，它们是游离的，酯化的或酰胺化的，并且它们的盐具有抗过敏和抗炎性质。它们例如通过使其中一个基团X5和X6是游离的或盐形式的羟基的另一种是由活性酯化的羟基或环氧基取代的烷氧基使式（Ⅰ）的化合物反应而制备。本发明还涉及其中R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素，R 11是氢或式R 1 -C（-O）的基团的式（ⅩⅩⅢ）中间体， - ，其中R1是低级烷基，及其盐。

8. 发明授权

US4670604A Novel fluorinated resorcinol ethers 失效
标题翻译：新型氟化间苯二酚醚
公开(公告)号：US4670604A
公开(公告)日：1987-06-02
申请号：US801012
申请日：1985-11-22
申请人： Andreas Beck , Alfred Sallmann , Robert W. Lang , Paul Wenk
发明人： Andreas Beck , Alfred Sallmann , Robert W. Lang , Paul Wenk
IPC分类号： C07C39/24 , C07C43/225 , C07C43/23 , C07C45/46 , C07C45/71 , C07C49/825 , C07C49/84 , C07C205/37 , C07D257/04
CPC分类号： C07D257/04 , C07C205/37 , C07C39/24 , C07C39/245 , C07C43/225 , C07C43/23 , C07C45/46 , C07C45/71 , C07C49/825 , C07C49/84
摘要： 4-Acylresorcinol ethers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties. They are prepared, for example, by reacting compounds of the formulae ##STR2## in which one of the radicals X.sub.5 and X.sub.6 is hydroxyl which is free or in salt form and the other is an alkoxy radical substituted by reactive esterified hydroxyl or epoxy. The invention also relates to intermediates of the formula ##STR3## in which R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen and R.sub.11 is hydrogen or a group of the formula R.sub.1 --O(.dbd.O)--, in which R.sub.1 is lower alkyl, and their salts.
摘要翻译：其中R 1是低级烷基，R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素的式（I）的4-间酰基间苯二酚醚，alk是不间断或中断的亚烷基或羟基亚烷基氧，基团R4，R5和R7之一是式-NH-C（= O）-R8的基团，与此不同的基团R 4或R 5是基团R 9和与此不同的基团R 7，基团R 10，R 6为氢，低级烷基，三氟甲基，卤素，羧基，其游离，酯化或酰胺化，氰基或低级烷酰基，R8为羧基，其为游离的，酯化的或酰胺化的或5-四唑基，R 9为氢，低级烷基，低级烷氧基，卤素或三氟甲基，R 10是氢，低级烷基，低级烷氧基，卤素，三氟甲基，氰基或羧基，它们是游离的，酯化的或酰胺化的，并且它们的盐具有抗过敏和抗炎性质。它们例如通过使式（IMAGE）的化合物与基团X5和X6中的一个是游离的或盐形式的羟基反应而制备，另一种是被反应性酯化的羟基或环氧基取代的烷氧基。本发明还涉及其中R 2是氟化的低级烷基，R 3是氢，低级烷氧基，三氟甲基或卤素，R 11是氢或式R 1 -O（= O）的基团的式（ⅩⅩⅢ）中间体， - ，其中R1是低级烷基，及其盐。

9. 发明授权

US4847258A Substituted benzoylphenylureas compounds useful as pesticides 失效
标题翻译：用作农药的取代苯甲酰基苯基化合物
公开(公告)号：US4847258A
公开(公告)日：1989-07-11
申请号：US86339
申请日：1987-08-17
申请人： Elmar Sturm , Robert W. Lang , Odd Kristiansen
发明人： Elmar Sturm , Robert W. Lang , Odd Kristiansen
IPC分类号： A01N47/34 , C07D239/34
CPC分类号： C07D239/34 , A01N47/34
摘要： The invention relates to novel N-benzoyl-N,-4-(5-phenylpyrimid-2-yloxy)phenylureas of formula ##STR1## wherein X.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio,X.sub.2 is halogen, methyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio,Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are each independently hydrogen, halogen, methyl, trifluoromethyl or methoxy,Z is methyl, halomethyl containing 1 to 3 halogen atoms or pentafluoroethyl; andR.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, trifluoromethyl or C.sub.1 -C.sub.3 alkoxy,to the preparation thereof and to intermediates for the synthesis of these compounds, as well as to compositions containing them for use in pest control, especially for controlling representatives of the order Acarina that attack plants and animals and for controlling insects. The novel compounds exhibit especially pronounced activity against plant-destructive mites.
摘要翻译：本发明涉及式（I）其中X 1为氢，卤素，C 1 -C 3烷氧基或C 1 -C 3烷硫基的新的N-苯甲酰基-N，4-（5-苯基嘧啶-2-基氧）苯基脲，X2 是卤素，甲基，C 1 -C 3烷氧基或C 1 -C 3烷硫基，Y 1，Y 2，Y 3和Y 4各自独立地为氢，卤素，甲基，三氟甲基或甲氧基，Z为甲基，含1至3个卤素原子的卤代甲基或五氟乙基; R 1，R 2和R 3各自独立地为氢，卤素，C 1 -C 3烷基，三氟甲基或C 1 -C 3烷氧基，并且用于合成这些化合物的中间体，以及含有它们用于病虫害防治的组合物，特别是控制攻击植物和动物并控制昆虫的蜱虫的代表。新型化合物对植物破坏性螨具有特别显着的活性。

10. 发明授权

US4822919A Novel production processes 失效
标题翻译：新型生产工艺
公开(公告)号：US4822919A
公开(公告)日：1989-04-18
申请号：US90200
申请日：1987-08-26
申请人： Pierre Martin , Robert W. Lang
发明人： Pierre Martin , Robert W. Lang
IPC分类号： A01N43/36 , A01N47/16 , C07C45/45 , C07C49/255 , C07D207/34 , C07C49/248
CPC分类号： C07D207/34 , A01N43/36 , A01N47/16 , C07C45/455 , C07C49/255
摘要： There is described a process for producing fungicidally active 4-phenylpyrrole derivatives of the formula I ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl, andn is 0, 1 or 2, which process comprises reacting a 3-trifluoromethyl-4-phenylpyrrole of the formula II ##STR2## wherein R.sub.n is as defined under the formula I, and R.sub.1 is hydrogen or an acyl group, at elevated temperature and elevated pressure, with ammonia. Important intermediates and the production thereof are also described.
摘要翻译：描述了制备式I的杀真菌活性4-苯基吡咯衍生物（I）的方法，其中R是卤素，C 1 -C 6烷基或C 1 -C 6 - 卤代烷基，n是0,1或2，其中方法包括在升高的温度和升高的压力下，使氨与式II的3-三氟甲基-4-苯基吡咯反应，其中Rn如式I所定义，R 1是氢或酰基。还描述了重要的中间体及其生产。

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