METHOD FOR PREPARING SUBSTITUTED BENZYL BROMIDES
    41.
    发明申请
    METHOD FOR PREPARING SUBSTITUTED BENZYL BROMIDES 审中-公开
    用于生产取代苄基溴化物

    公开(公告)号:WO99006339A1

    公开(公告)日:1999-02-11

    申请号:PCT/EP1998/004485

    申请日:1998-07-20

    Abstract: The invention concerns a method for preparing substituted benzyl bromides of general formula (I), wherein at least one substituent R represents an electroattractive group, such as fluorine, chlorine, bromine, C1-C4 alkoxycarbonyl, cyano or nitro, and the remaining R substituents represent hydrogen or methyl, by bromination of substituted toluenes of general formula (II) with a bromination agent at temperatures from 20 to 95 DEG C.

    Abstract translation: 一种用于制备通式(I),其中至少一个取代基R <1-5>表示吸电子基团如氟,氯,溴,C1-C4烷氧羰基,氰基或硝基,其余取代基R的取代的苄基溴化物过程< 意味着1-5>氢或甲基,通过在从20℃至95℃的式(II)用溴化剂的取代的甲苯的溴化

    3-CYANO-2,4,5-TRIFLUORO-BENZOYL FLUORIDE AND INTERMEDIATE PRODUCTS FOR THE PRODUCTION THEREOF
    42.
    发明申请
    3-CYANO-2,4,5-TRIFLUORO-BENZOYL FLUORIDE AND INTERMEDIATE PRODUCTS FOR THE PRODUCTION THEREOF 审中-公开
    3-氰基2,4,5三氟苯甲酰及其生产中间产品

    公开(公告)号:WO98047862A1

    公开(公告)日:1998-10-29

    申请号:PCT/EP1998/002175

    申请日:1998-04-14

    Abstract: The invention relates to 3-cyano-2,4,5-trifluoro-benzoyl fluoride and intermediate products for the production thereof and a method for the production of 3-cyano-2,4,5-trifluoro-benzoyl fluoride starting from 5-fluoro-1,3-xylol (VIII), which is chlorinated twice in the presence of a catalyst with ionic conditions in the nucleus to obtain 2,4-dichloro-5-fluoro-1,3-dymethylbenzol (VII), which is then chlorinated with radical conditions in the side chains to obtain 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethyl benzol (VI), which is subsequently saponified by the optionally isolatable 2,4-dichloro-5-fluoro-3-dichloromethyl benzoic acid (V) to obtain 2,4-dichloro-5-fluoro-3-formyl-benzoic acid (IV) whose aldehyde group is converted to 2,4-dichloro-5-fluoro-3-N-hydroxyiminomethyl-benzoic acid (III), whereupon water is eliminated using an acid chloride while at the same time converting the carboxyl group into a chlorocarbonyl group to obtain nitrile 2,4-dichloro-3-cyano-5-fluoro-benzoyl-chloride (II), which is finally subjected to a fluorine/chlorine exchange.

    Abstract translation: 本发明涉及到3-氰基-2,4,5-三氟苯甲酰氟(I)和它的制备的中间体和用于制备3-氰基-2,4,5-三氟苯甲酰氟,5-氟过程 1,3-二甲苯(VIII)进行,其中在催化剂的存在下双氯化离子条件下在核心,得到2,4-二氯-5-氟-1,3-二甲基苯(VII)。 这是在侧链自由基条件下氯化,得到2,4-二氯-5-氟-3-二氯-1-三氯甲苯(VI)。 这是任选皂化绝缘2,4-二氯-5-氟-3-dichlormethylbenzoesäure(V),得到2,4-二氯-5-氟-3-甲酰基 - 苯甲酸(IV),醛基是2, 2,4-二氯-5-氟 - 3-N-羟基亚 - 苯甲酸(III)反应,并在同一时间将羧基转化成氯基团时,水从这些使用酰氯,得到腈2,4-二氯-3-氰基 - 形成, 5-氟 - 苯甲酰氯(II)被消除。 这是最后进行氟/氯交换。

    AF4 SYNTHESIS
    43.
    发明申请
    AF4 SYNTHESIS 审中-公开
    AF4合成

    公开(公告)号:WO98041490A1

    公开(公告)日:1998-09-24

    申请号:PCT/US1998/003654

    申请日:1998-02-25

    CPC classification number: C07C17/14 C07C17/269 C07C2603/92 C07C22/08 C07C23/18

    Abstract: Methods of making AF4 using novel reducing agents that result in reduced cost. Low dilution technology may be used to provide AF4 in substantially improved yields. The relative amount of transition metal catalyst can be decreased. The amount of undesired byproduct is also reduced.

    Abstract translation: 使用降低成本的新型还原剂制备AF4的方法。 可以使用低稀释技术来以显着提高的产率提供AF4。 过渡金属催化剂的相对量可以降低。 不希望的副产物的量也减少了。

    AMIDE DERIVATIVES AND THEIR THERAPEUTIC USE
    45.
    发明申请
    AMIDE DERIVATIVES AND THEIR THERAPEUTIC USE 审中-公开
    酰胺衍生物及其治疗用途

    公开(公告)号:WO1995030645A1

    公开(公告)日:1995-11-16

    申请号:PCT/GB1995001040

    申请日:1995-05-09

    Abstract: A compound of formula (I), wherein R and R are independently selected from chloro, fluoro, bromo, C1-6 alkyl, C1-6 alkoxy or C1-6 haloalkyl provided that both R and R are not fluoro; R and R are independently selected from hydrogen and C1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.

    Abstract translation: 式(I)化合物,其中R 1和R 2独立地选自氯,氟,溴,C 1-6烷基,C 1-6烷氧基或C 1-6卤代烷基,条件是R 1和 R 2不是氟; R 3和R 4独立地选自氢和C 1-6烷基,及其药学上可接受的盐,溶剂合物或生理功能衍生物,它们在药物中的用途,特别是肺炎或治疗与炎症,关节炎, 或疼痛,包含它们的药物组合物及其制备方法。

    塔式连续光氯化法制氯苄
    47.
    发明申请

    公开(公告)号:WO2018214642A1

    公开(公告)日:2018-11-29

    申请号:PCT/CN2018/080985

    申请日:2018-03-29

    CPC classification number: B01J19/12 C07B39/00 C07C17/14

    Abstract: 本发明涉及塔式连续光氯化法制氯苄,使化学式为(X) a C 6 H 6-a-b (CH 3 ) b 的芳烃类化合物在流动中成液膜,与氯气在光照条件下进行膜界面光氯化反应,反应开始时侧链甲基上的一个氢被氯取代生成一氯苄。并可以继续通入氯气反应,苄基上的两个氢被氯取代生成二氯苄,以此类推,侧链甲基上的氢逐渐被氯取代,并最终可以得到侧链甲基上的氢全部被氯取代的产物。本申请的主要优点在于:副反应少,产品收率高,产品纯度高,且易于进一步纯化,反应效率高,生产时间短,适宜于工业化生产。

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