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81. 发明申请

US20050239799A1 1-phenyl-4-benzylpiperazines dopamine receptor subtype 失效
标题翻译： 1-苯基-4-苄基哌嗪多巴胺受体亚型
公开(公告)号：US20050239799A1
公开(公告)日：2005-10-27
申请号：US11167735
申请日：2005-06-27
申请人： Andrew Thurkauf , Xi Chen
发明人： Andrew Thurkauf , Xi Chen
IPC分类号： C07D295/06 , A61K31/495 , A61P25/18 , A61P43/00 , C07D241/04 , C07D295/073 , C07D295/08 , C07D295/096 , C07D295/112 , C07D295/135 , C07D317/58 , C07D319/18
CPC分类号： C07D295/073 , A61K31/495 , C07C2603/08 , C07D295/096 , C07D295/112 , C07D295/135
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1-C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, hydroxy, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.
摘要翻译：公开了下式的化合物或其药学上可接受的加成盐，其中：R 1是卤素或C 1 -C 4烷基; R 2和R 3相同或不同，表示氢，卤素，C 1 -C 4烷基，烷基，C 1 -C 4烷氧基，烷硫基，羟基，氨基，单（C 1 -C 4 - ）烷基氨基，二（C 1 -C 4 - ）烷基氨基或R 2和R 3一起代表一个与它们所连接的苯环一起形成萘基部分的4碳亚烯基部分，该化合物可用于治疗神经疾病疾病如精神分裂症，精神病抑郁症和躁狂症。

82. 发明申请

US20050234058A1 Secondary amino-and cycloamino-cycloalkanol derivatives and methods of their use 失效
标题翻译：仲氨基和环氨基 - 环烷醇衍生物及其使用方法
公开(公告)号：US20050234058A1
公开(公告)日：2005-10-20
申请号：US10962899
申请日：2004-10-12
申请人： Paige Mahaney , Michael Webb , Lori Gavrin , Eugene Trybulski
发明人： Paige Mahaney , Michael Webb , Lori Gavrin , Eugene Trybulski
IPC分类号： A61K31/137 , A61K31/445 , A61K31/537 , C07C215/42 , C07D207/14 , C07D209/16 , C07D211/06 , C07D211/46 , C07D211/58 , C07D213/38 , C07D215/12 , C07D265/32 , C07D295/073 , C07D295/088 , C07D295/096 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/58 , C07D471/04
CPC分类号： C07C215/42 , C07C2601/04 , C07C2601/14 , C07D207/14 , C07D209/16 , C07D211/46 , C07D211/58 , C07D213/38 , C07D215/12 , C07D295/073 , C07D295/088 , C07D295/096 , C07D307/52 , C07D307/81 , C07D309/10 , C07D317/58 , C07D333/28 , C07D333/58 , C07D471/04
摘要： The present invention is directed to secondary amino- and cycloamino-cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
摘要翻译：本发明涉及仲氨基和环氨基 - 环烷醇衍生物，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS），性功能障碍，特别是选自重度抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛，糖尿病性神经病变以及纤维肌痛症状其组合。

83. 发明申请

US20050182069A1 Enantiomers of 1-[(4-chlorophenyl) phenylmethyl]-4-[(4-methylphenyl) sulfonyl] piperazine 审中-公开
标题翻译： 1 - [（4-氯苯基）苯基甲基] -4 - [（4-甲基苯基）磺酰基]哌嗪的对映异构体
公开(公告)号：US20050182069A1
公开(公告)日：2005-08-18
申请号：US11106528
申请日：2005-04-15
申请人： Eric Cossement , Guy Bodson , Jean Gobert
发明人： Eric Cossement , Guy Bodson , Jean Gobert
IPC分类号： C07D295/06 , A61K31/495 , A61P11/06 , A61P25/20 , A61P25/22 , A61P29/00 , A61P37/08 , A61P43/00 , C07B53/00 , C07D295/04 , C07D295/073 , C07D295/08 , C07D295/088 , C07D295/22 , C07D295/26
CPC分类号： A61K31/495 , C07D295/073 , C07D295/088 , C07D295/26
摘要： Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl)-4-[(4-methylphenyl)sulfonyl]piperazine of the formula their preparation and use for the preparation of substantially optically pure enantiomers of 1-1(4-chlorophenyl)phenylmethyl]piperazine, which are themselves valuable intermediate products for the preparation of optically active therapeutic compounds having a very high degree of optical purity.
摘要翻译：具有下式的1 - [（4-氯苯基）苯基甲基）-4 - [（4-甲基苯基）磺酰基]哌嗪的左旋和右旋对映异构体的制备和用途，用于制备1-1（4-氯苯基））苯甲基]哌嗪，其本身是用于制备具有非常高的光学纯度的光学活性治疗化合物的有价值的中间产物。

84. 发明授权

US06924374B2 Modulators of dopamine neurotransmission 有权
公开(公告)号：US06924374B2
公开(公告)日：2005-08-02
申请号：US10168019
申请日：2000-12-22
申请人： Clas Sonesson , Ingela Marianne Svan , Susanna Waters , Nicholas Waters , Joakim Tedroff
发明人： Bengt Andersson
IPC分类号： C07D295/06 , A61K31/4409 , A61K31/451 , A61K31/495 , A61P3/04 , A61P15/10 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D211/18 , C07D211/24 , C07D211/34 , C07D211/70 , C07D241/04 , C07D295/073 , C07D295/08 , C07D295/096 , C07D295/12 , C07D295/14 , C07D211/04 , A61K31/445
CPC分类号： C07D295/073 , C07D211/18 , C07D241/04 , C07D295/096
摘要： New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bind at the dotted line; R1 is CF3, OSO2CF3, OSO2CH3, SOR7, SO2R7, COR7, CN, OR3, NO2, CONHR3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, and NH2; R3 and R4 are independently H or a C1-C4 alkyl; R5 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)R6; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetra-hydrofurane; R7 is a C1-C3 alkyl, CF3, or N(R4)2, and pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

85. 发明授权

US06894052B1 Diarylalkylpiperazines active on the lower urinary tract 失效
标题翻译：在下尿路上活性的二芳基烷基哌嗪
公开(公告)号：US06894052B1
公开(公告)日：2005-05-17
申请号：US09127059
申请日：1998-07-31
申请人： Amedeo Leonardi , Gianni Motta , Carlo Riva , Rodolfo Testa
发明人： Amedeo Leonardi , Gianni Motta , Carlo Riva , Rodolfo Testa
IPC分类号： C07D295/08 , A61K31/495 , A61K31/496 , A61P13/00 , A61P25/00 , A61P43/00 , C07D213/38 , C07D213/40 , C07D213/56 , C07D213/57 , C07D213/74 , C07D295/096 , C07D295/15 , C07D319/18 , C07D401/14 , C07D295/073 , C07D403/14
CPC分类号： C07D295/096 , A61K31/495 , A61K31/496 , C07D213/38 , C07D213/56 , C07D213/57 , C07D295/15 , C07D319/18 , C07D401/14
摘要： Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.
摘要翻译：本文公开了用于治疗下尿路疾病的新型化合物和方法。新化合物是二芳基烷基哌嗪衍生物。所述方法包括施用本发明的新化合物和结合5HT 1A受体的其它化合物，用于治疗下泌尿道疾病。

86. 发明授权

US06867298B2 Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳 - 杂原子和碳 - 碳键
公开(公告)号：US06867298B2
公开(公告)日：2005-03-15
申请号：US10435719
申请日：2003-05-08
申请人： Stephen L. Buchwald , Artis Klapars , Jon C. Antilla , Gabriel E. Job , Martina Wolter , Fuk Y. Kwong , Gero Nordmann , Edward J. Hennessy
发明人： Stephen L. Buchwald , Artis Klapars , Jon C. Antilla , Gabriel E. Job , Martina Wolter , Fuk Y. Kwong , Gero Nordmann , Edward J. Hennessy
IPC分类号： B01J31/26 , C07B37/04 , C07B41/04 , C07B43/04 , C07B61/00 , C07C41/16 , C07C41/24 , C07C43/15 , C07C43/20 , C07C43/23 , C07C45/68 , C07C45/71 , C07C49/84 , C07C51/353 , C07C59/64 , C07C67/343 , C07C69/612 , C07C209/10 , C07C211/48 , C07C211/53 , C07C211/54 , C07C213/02 , C07C213/08 , C07C215/16 , C07C215/70 , C07C217/48 , C07C217/82 , C07C221/00 , C07C227/08 , C07C227/18 , C07C229/56 , C07C231/08 , C07C231/12 , C07C233/07 , C07C233/25 , C07C233/40 , C07C233/51 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/80 , C07C233/81 , C07C237/40 , C07C241/04 , C07C243/38 , C07C249/02 , C07C249/16 , C07C251/18 , C07C251/86 , C07C253/14 , C07C253/30 , C07C255/23 , C07C269/06 , C07C271/28 , C07C273/18 , C07C275/32 , C07C277/08 , C07C279/18 , C07C281/02 , C07C303/38 , C07C311/21 , C07C319/20 , C07C323/41 , C07D205/08 , C07D207/16 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/32 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/65 , C07D213/74 , C07D215/38 , C07D221/12 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/34 , C07D233/58 , C07D235/06 , C07D235/08 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D273/08 , C07D295/02 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07D521/00 , C07F9/38 , C07F9/40 , C07D273/02 , C07D267/02 , C07D281/02 , C07D285/36
CPC分类号： C07F9/4056 , C07B37/04 , C07B41/04 , C07B43/04 , C07C41/16 , C07C45/68 , C07C45/71 , C07C51/353 , C07C67/343 , C07C209/10 , C07C213/08 , C07C221/00 , C07C227/18 , C07C231/08 , C07C231/12 , C07C241/04 , C07C249/02 , C07C249/16 , C07C253/14 , C07C253/30 , C07C269/06 , C07C273/1854 , C07C277/08 , C07C281/02 , C07C303/38 , C07C319/20 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/08 , C07D207/16 , C07D207/267 , C07D207/27 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/74 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D235/06 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07C49/84 , C07C59/68 , C07C69/76 , C07C69/65 , C07C69/612 , C07C69/734 , C07C69/616 , C07C69/732 , C07C311/21 , C07C323/41 , C07C211/48 , C07C211/52 , C07C211/55 , C07C211/54 , C07C215/68 , C07C217/84 , C07C215/16 , C07C225/22 , C07C217/08 , C07C229/56 , C07C229/60 , C07C211/58 , C07C243/38 , C07C251/86 , C07C43/205 , C07C43/2055 , C07C43/235 , C07C43/23 , C07C43/16 , C07C43/215 , C07C43/225 , C07C237/30 , C07C255/58 , C07C233/07
摘要： The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.
摘要翻译：本发明涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在酰胺或胺部分的氮原子与芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 氮键的铜催化方法。在另外的实施方案中，本发明涉及在酰基肼的氮原子和芳基，杂芳基或卤乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜催化方法。在其它实施方案中，本发明涉及在含氮杂芳族化合物（例如吲哚，吡唑和吲唑）的氮原子与芳基，杂芳基的活性炭之间形成碳 - 氮键的铜催化方法，或乙烯基卤化物或磺酸盐。在某些实施方案中，本发明涉及在醇的氧原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 氧键的铜催化方法。本发明还涉及在包含亲核性碳原子的反应物（例如烯醇化物或丙二酸酯阴离子）和芳基，杂芳基或卤乙烯或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。重要的是，由于催化剂所含的铜的低成本，本发明的所有方法都相对便宜。

87. 发明授权

US6124476A Catalyst ligands, catalyst compositions, catalyst metal complexes and processes for cross-coupling aromatic boron compounds with aromatic halogens or perfluoroalkylsulfonates 有权
标题翻译：催化剂配体，催化剂组合物，催化剂金属络合物和芳香族硼化合物与芳族卤素或全氟烷基磺酸盐交叉偶联的方法
公开(公告)号：US6124476A
公开(公告)日：2000-09-26
申请号：US252182
申请日：1999-02-18
申请人： Anil Guram , Xiaohong Bei , Timothy S. Powers , Bernd Jandeleit , Thomas Crevier
发明人： Anil Guram , Xiaohong Bei , Timothy S. Powers , Bernd Jandeleit , Thomas Crevier
IPC分类号： B01J31/24 , C07B61/00 , C07C209/10 , C07C211/48 , C07D295/023 , C07D295/073 , C07F9/50 , C07F9/655 , C07F15/00 , C07D321/00 , C07D307/02 , C07F9/02
CPC分类号： C07F9/65515 , B01J31/2247 , B01J31/2404 , B01J31/2447 , C07C209/10 , C07D295/023 , C07D295/073 , C07F15/0066 , C07F9/5018 , C07F9/5022 , B01J2231/4211 , B01J2531/821 , B01J2531/824 , B01J2531/827 , B01J2531/828 , B01J2531/84
摘要： The present invention discloses new organic compounds (e.g., ligands), their metal complexes and compositions using those compounds. The invention also relates to the field of catalysis. In particular, this invention relates to new compounds which when combined with suitable metals or metal precursor compounds provide useful catalysts for various bond-forming reactions, including Suzuki cross-coupling reactions. The invention also relates to performing Suzuki cross coupling reactions with unreactive aryl-chlorides.
摘要翻译：本发明公开了新的有机化合物（例如配体），它们的金属络合物和使用这些化合物的组合物。本发明还涉及催化领域。特别地，本发明涉及当与合适的金属或金属前体化合物组合时提供用于各种形成结合反应（包括Suzuki交叉偶联反应）的有用催化剂的新化合物。本发明还涉及用非反应性芳基氯化物进行Suzuki交叉偶联反应。

88. 发明授权

US6057323A Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith 失效
标题翻译：卡帕激动剂化合物药物制剂及其预防和治疗瘙痒的方法
公开(公告)号：US6057323A
公开(公告)日：2000-05-02
申请号：US183011
申请日：1998-10-30
申请人： Wei Yuan Zhang , Alan L. Maycock , Michael Anthony Marella , Virendra Kumar , Forrest Gaul , An-Chih Chang , Deqi Guo
发明人： Wei Yuan Zhang , Alan L. Maycock , Michael Anthony Marella , Virendra Kumar , Forrest Gaul , An-Chih Chang , Deqi Guo
IPC分类号： A61K31/404 , A61K31/4439 , A61K45/06 , C07D207/12 , C07D209/42 , C07D213/56 , C07D241/04 , C07D295/073 , C07D403/06 , A61K31/495
CPC分类号： A61K31/404 , A61K31/4439 , A61K45/06 , C07D207/12 , C07D209/42 , C07D213/56 , C07D241/04 , C07D295/073 , C07D403/06
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X; and ArY, Z and n are as described in the specification.
摘要翻译：提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。具有以下结构的式I化合物：其中R1，R2; X; Ar Y，Z和n如说明书中所述。

89. 发明授权

US6054445A Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritis therewith 失效
标题翻译：卡帕激动剂化合物药物制剂及其预防和治疗瘙痒的方法
公开(公告)号：US6054445A
公开(公告)日：2000-04-25
申请号：US307387
申请日：1999-05-07
申请人： Wei Yuan Zhang , Alan L. Maycock , Michael Anthony Marella , Virendra Kumar , Forrest Gaul , An-Chih Chang , Deqi Guo
发明人： Wei Yuan Zhang , Alan L. Maycock , Michael Anthony Marella , Virendra Kumar , Forrest Gaul , An-Chih Chang , Deqi Guo
IPC分类号： A61K31/404 , A61K31/4439 , A61K45/06 , C07D207/12 , C07D209/42 , C07D213/56 , C07D241/04 , C07D295/073 , C07D403/06 , A61K31/675 , A61K31/40
CPC分类号： A61K31/404 , A61K31/4439 , A61K45/06 , C07D207/12 , C07D209/42 , C07D213/56 , C07D241/04 , C07D295/073 , C07D403/06
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formulae IIA, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X.sub.4, X.sub.5 ; andAr and n are as described in the specification.
摘要翻译：提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。具有以下结构的式IIA化合物：其中R1，R2; X4，X5; Ar和n如说明书中所述。

90. 发明授权

US5990309A 2-chloro-5-fluoro-4-morpholinonitrobenzene and 2-chloro-5-fluoro-4-morpholinoaniline 失效
标题翻译： 2-氯-5-氟-4-吗啉代硝基苯和2-氯-5-氟-4-吗啉代苯胺
公开(公告)号：US5990309A
公开(公告)日：1999-11-23
申请号：US272839
申请日：1999-03-19
申请人： Thomas Schach , Theodor Papenfuhs
发明人： Thomas Schach , Theodor Papenfuhs
IPC分类号： C07D295/06 , C07B61/00 , C07C269/00 , C07C269/04 , C07C271/28 , C07D295/073 , C07D295/135 , C07D295/04
CPC分类号： C07D295/073 , C07C269/00 , C07C269/04 , C07D295/135
摘要： The present invention relates to a process for the preparation of N-carboxyalkyl-3-fluoro-4-dialkylaminoanilines, which comprises reacting, in a first step, an ortho-nitrochlorobenzene of the formula (1) in which X is Cl or F, with a secondary amine of the formula (2) HNR.sup.1 R.sup.2, in which R.sup.1 and R.sup.2, independently of one another, are identical or different and are an alkyl radical having from 1 to 10 carbon atoms or, together with the N atom to which they are bonded, form a ring having from 3 to 7 members, in the presence of a base in the presence or absence of a solvent at from -10 to 120.degree. C., reacting, in a second step, the 2-chloro-4-dialkylamino-5-fluoronitrobenzene with hydrogen at from 30 to 150.degree. C. and from 1 to 100 bar in the presence of a base and a noble-metal catalyst and, in a third step, extracting the 3-fluoro-4-dialkylaminoaniline from the reaction mixture using an aqueous solution of an acid as a salt dissolved in water, removing the aqueous phase and reacting the 3-fluoro-4-dialkylaminoaniline salt, dissolved in water, with a chloroformate of the formula (3) ClCO.sub.2 R.sup.3, in which R.sup.3 is an alkyl radical having from 1 to 10 carbon atoms or an aralkyl radical having from 7 to 20 carbon atoms, at from 0 to 100.degree. C. in the presence of a basic compound.
摘要翻译：本发明涉及N-羧基烷基-3-氟-4-二烷基氨基苯胺的制备方法，其包括在第一步中使式（1）的邻硝基氯苯（其中X为Cl或F）与式（2）HNR1R2的仲胺，其中R 1和R 2彼此独立地相同或不同，并且是具有1至10个碳原子的烷基或与它们相同的N原子在存在或不存在溶剂的情况下，在-10至120℃下，在碱的存在下形成具有3至7个成员的环，在第二步中，将2-氯-4- 二烷基氨基-5-氟硝基苯，在碱和贵金属催化剂的存在下，在30至150℃和1至100巴的氢气下进行，并且在第三步骤中，将3-氟-4-二烷基氨基苯胺从所述反应混合物使用溶于水的盐的酸的水溶液，除去所述水相并使所述3-氟 - （3）ClCO 2 R 3的氯甲酸酯（其中R 3是具有1至10个碳原子的烷基或具有7至20个碳原子的芳烷基）溶于水中的4-氟-4-二烷基氨基苯胺盐，在碱性化合物的存在下0至100℃。

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