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    Friedel-crafts-acylierung zur Synthese von Aryl- und Heteroaryl-(3-ethyl-4-nitro-phenyl)-Methanonen
    2.
    发明公开
    Friedel-crafts-acylierung zur Synthese von Aryl- und Heteroaryl-(3-ethyl-4-nitro-phenyl)-Methanonen 有权
    Friedel-crafts-acylierung zur Synthese von Aryl- und Heteroaryl-（3-乙基-4-硝基 - 苯基）-Methanonen

    公开(公告)号：EP2311792A1

    公开(公告)日：2011-04-20

    申请号：EP09012899.2

    申请日：2009-10-13

    Applicant: Roche Diagnostics GmbH ,  F.Hoffmann-La Roche AG

    Inventor： Knipp, Bernhard

    IPC: C07C201/12 ,  C07C205/45

    CPC classification number: C07C201/12 ,  C07C205/45 ,  C07D317/18 ,  C07D319/06

    Abstract: Die vorliegende Erfindung betrifft ein Syntheseverfahren enthaltend die folgenden Schritte (i) Umsetzung von 3-Ethyl-4-nitrobenzoesäure mit Thionylchlorid zur Erzeugung eines 3-Ethyl-4-nitrobenzoesäurechlorids oder mittels Wasserabspaltung aus 3-Ethyl-4-nitrobenzoesäure eines 3-Ethyl-4-nitrobenzoesäureanhydrids und (ii) Friedel-Crafts-Acylierung durch Reaktion des 3-Ethyl-4-nitrobenzoesäurechlorids oder des 3-Ethyl-4-nitrobenzoesäureanhydrids mit gegebenenfalls substituiertem Aryl-H, so dass gegebenenfalls substituiertes (3-Ethyl-4-nitrophenyl)-aryl-methanon entsteht. Darüber hinaus betrifft die vorliegende Erfindung Verbindungen enthaltend (3-Ethyl-4-nitrophenyl)-aryl-methanon, dadurch gekennzeichnet, dass das gegebenenfalls substituierte Aryl ein gegebenenfalls substituierter kondensierter Aromat ist.

    Abstract translation: 合成方法包括：（a）使3-乙基-4-硝基苯甲酸与亚硫酰卤反应生成3-乙基-4-硝基苯甲酰卤; 和（b）通过使3-乙基-4-硝基苯甲酰氯或3-乙基-4-硝基苯甲酸酐与任选取代的芳基-H反应形成任选取代的（3-乙基-4-硝基苯甲酸） 硝基 - 苯基） - 芳基 - 甲酮。 包括独立权利要求：（1）（3-乙基-4-硝基苯基） - 芳基 - 甲酮或[3-（2-羟基-1-甲基 - 乙基）-4-硝基苯基] - 芳基 - 甲酮，其中 芳基是稠合的芳族化合物，其任选被取代; 和（2）在5'或3'位置含有取代基的核苷，其中取代基是[3-（2-O-1-甲基 - 乙基）-4-硝基苯基] - 芳基 - 甲酮。

    PESTICIDES
    4.
    发明授权
    PESTICIDES 失效
    农药

    公开(公告)号：EP0738260B2

    公开(公告)日：2006-12-13

    申请号：EP95905110.3

    申请日：1994-12-27

    Applicant: Bayer CropScience AG

    Inventor： ZIEGLER, Hugo ,  TRAH, Stephan ,  FAROOQ, Saleem ,  ZURFLÜH, René

    IPC: C07C251/60 ,  A01N37/00

    CPC classification number: C07D213/77 ,  A01N37/36 ,  A01N37/50 ,  A01N43/28 ,  A01N43/30 ,  A01N43/36 ,  A01N43/40 ,  A01N43/46 ,  A01N43/653 ,  A01N43/84 ,  A01N55/00 ,  C07C251/60 ,  C07C251/76 ,  C07C251/80 ,  C07C255/54 ,  C07C255/61 ,  C07C2601/02 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/088 ,  C07D295/30 ,  C07D317/18 ,  C07D317/58 ,  C07D333/22

    Abstract: Compounds of formula (I) and the isomers, and isomer mixtures thereof, which are possible, in which either a) X is an N atom and Y is OR11 or N(R12)R13, or b) X is CH and Y is OR11, and in which furthermore: R11 is C1-C4alkyl; R12 and R13, independently, are hydrogen or C1-C4alkyl; A is an O atom or the group NR4; R1 is hydrogen, C1-C4alkyl, halo-C1-C4alkyl, cyclopropyl, cyano or methylthio; R2 is hydrogen, C1-C6alkyl, C3-C6cycloalkyl, a group (i), a group (ii), or thienyl; R3 is hydrogen, C1-C6alkyl, C1-C6haloalkyl having 1 to 5 halogen atoms, C1-C4alkoxy-C1-C2alkyl, C2-C4alkenyl-C1-C2alkyl, which is unsubstituted or substituted by 1 to 3 halogen atoms, C2-C4alkynyl-C1-C2-alkyl, C3-C6cycloalkyl which is unsubstituted or substituted by 1 to 4 halogen atoms, C3-C6-cycloalkyl-C1-C4alkyl which is unsubstituted or substituted by 1 to 4 halogen atoms, cyano-C1-C4alkyl; C1-C4alkoxycarbonyl-C1-C2alkyl, C1-C4alkoxycarbamoyl-C1-C2alkyl, phenyl-C1-C3alkyl which is unsubstituted or substituted by halogen, C1-C3alkyl, C1-C4alkoxy, C1-C4haloalkyl, cyano, nitro or C1-C4alkylenedioxy, it being possible for the phenyl group to be monosubstituted to trisubstituted by identical or different substituents; phenyl which is unsubstituted or mono- to disubstituted, independently, by C1-C4alkyl, C1-C4alkoxy, halogen, C1-C2haloalkyl having 1 to 3 halogen atoms, nitro or cyano, or pyridyl which is unsubstituted or mono- to disubstituted, independently, by C1-C4alkyl, C1-C4alkoxy, halogen, C1-C2haloalkyl having 1 to 3 halogen atoms, nitro or cyano; R4 is C1-C4alkyl, phenyl, or R3 and R4 together with the nitrogen atom to which they are bonded form a saturated or unsaturated 5- to 7-membered ring which is unsubstituted or substituted by C1-C4alkyl and which can have 1 to 3 additional hetero atoms selected from amongst N, O and S, and in which the substituents Z, B, D and n are as defined in the present publication, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.

    SULFONYL UREA DERIVATIVES AND THEIR USE IN THE CONTROL OF INTERLEUKIN-1 ACTIVITY
    6.
    发明公开
    SULFONYL UREA DERIVATIVES AND THEIR USE IN THE CONTROL OF INTERLEUKIN-1 ACTIVITY 失效
    苏黎世自然保护联盟

    公开(公告)号：EP0964849A1

    公开(公告)日：1999-12-22

    申请号：EP97947201.0

    申请日：1997-12-29

    Applicant: PFIZER INC.

    Inventor： DOMBROSKI, Mark, Anthony ,  EGGLER, James, Frederick

    IPC: C07D233 ,  A61K31 ,  A61P1 ,  A61P9 ,  A61P19 ,  A61P25 ,  A61P29 ,  A61P37 ,  C07C311 ,  C07C317 ,  C07C323 ,  C07D209 ,  C07D235 ,  C07D307 ,  C07D317 ,  C07D333 ,  C07D335 ,  C07D407 ,  C07D409

    CPC classification number: C07D307/64 ,  C07C311/60 ,  C07C317/14 ,  C07C323/67 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/08 ,  C07D317/18 ,  C07D333/34

    Abstract: A compound of formula (I) wherein R?1 and R2¿ are as defined in the description, R2 being an aromatic group, useful in the treatment and condition selected from the group consisting of the group meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzeimer's disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including a human.

    Abstract translation: PCT No.PCT / IB97 / 01603 Sec。 371日期：1999年7月16日 102（e）1999年7月16日PCT 1997年12月29日PCT公布。 公开号WO98 / 32733 日期：1998年7月30日其中R1和R2如说明书中所定义的式（I）化合物，R2为芳族基团，可用于治疗和选自组脑膜炎和输卵管炎，败血性休克， 弥漫性血管内凝血和/或成人呼吸窘迫综合征，急性或慢性炎症，关节炎，胆管炎，结肠炎，脑炎，心内膜炎，肾小球性肾炎，肝炎，心肌炎，胰腺炎，心包炎，再灌注损伤，血管炎，急性和迟发型超敏反应， 和移植物抗宿主病，自身免疫性疾病，包括1型糖尿病和多发性硬化，牙周病，间质性肺纤维化，肝硬化，系统性硬化，产生IL-1作为自分泌生长因子的瘢痕疙瘩形成肿瘤，恶病质，Alzeimer's 疾病，打击乐伤害，抑郁症，动脉粥样硬化，哺乳动物，包括人类的骨质疏松症。

    PESTICIDES
    8.
    发明公开
    PESTICIDES 失效
    农药

    公开(公告)号：EP0738260A1

    公开(公告)日：1996-10-23

    申请号：EP95905110.0

    申请日：1994-12-27

    Applicant: CIBA-GEIGY AG

    Inventor： ZIEGLER, Hugo ,  TRAH, Stephan ,  FAROOQ, Saleem ,  ZURFLÜH, René

    IPC: A01N37 ,  A01N43 ,  A01N55 ,  C07C229 ,  C07C251 ,  C07C255 ,  C07D213 ,  C07D295 ,  C07D317 ,  C07D333 ,  C07D521

    CPC classification number: C07D213/77 ,  A01N37/36 ,  A01N37/50 ,  A01N43/28 ,  A01N43/30 ,  A01N43/36 ,  A01N43/40 ,  A01N43/46 ,  A01N43/653 ,  A01N43/84 ,  A01N55/00 ,  C07C251/60 ,  C07C251/76 ,  C07C251/80 ,  C07C255/54 ,  C07C255/61 ,  C07C2601/02 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/088 ,  C07D295/30 ,  C07D317/18 ,  C07D317/58 ,  C07D333/22

    Abstract: Compounds of formula (I) and the isomers, and isomer mixtures thereof, which are possible, in which either a) X is an N atom and Y is OR11 or N(R12)R13, or b) X is CH and Y is OR11, and in which furthermore: R11 is C1-C4alkyl; R12 and R13, independently, are hydrogen or C1-C4alkyl; A is an O atom or the group NR4; R1 is hydrogen, C1-C4alkyl, halo-C1-C4alkyl, cyclopropyl, cyano or methylthio; R2 is hydrogen, C1-C6alkyl, C3-C6cycloalkyl, a group (i), a group (ii), or thienyl; R3 is hydrogen, C1-C6alkyl, C1-C6haloalkyl having 1 to 5 halogen atoms, C1-C4alkoxy-C1-C2alkyl, C2-C4alkenyl-C1-C2alkyl, which is unsubstituted or substituted by 1 to 3 halogen atoms, C2-C4alkynyl-C1-C2-alkyl, C3-C6cycloalkyl which is unsubstituted or substituted by 1 to 4 halogen atoms, C3-C6-cycloalkyl-C1-C4alkyl which is unsubstituted or substituted by 1 to 4 halogen atoms, cyano-C1-C4alkyl; C1-C4alkoxycarbonyl-C1-C2alkyl, C1-C4alkoxycarbamoyl-C1-C2alkyl, phenyl-C1-C3alkyl which is unsubstituted or substituted by halogen, C1-C3alkyl, C1-C4alkoxy, C1-C4haloalkyl, cyano, nitro or C1-C4alkylenedioxy, it being possible for the phenyl group to be monosubstituted to trisubstituted by identical or different substituents; phenyl which is unsubstituted or mono- to disubstituted, independently, by C1-C4alkyl, C1-C4alkoxy, halogen, C1-C2haloalkyl having 1 to 3 halogen atoms, nitro or cyano, or pyridyl which is unsubstituted or mono- to disubstituted, independently, by C1-C4alkyl, C1-C4alkoxy, halogen, C1-C2haloalkyl having 1 to 3 halogen atoms, nitro or cyano; R4 is C1-C4alkyl, phenyl, or R3 and R4 together with the nitrogen atom to which they are bonded form a saturated or unsaturated 5- to 7-membered ring which is unsubstituted or substituted by C1-C4alkyl and which can have 1 to 3 additional hetero atoms selected from amongst N, O and S, and in which the substituents Z, B, D and n are as defined in the present publication, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.

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