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    PROCESS FOR THE PREPARATION OF 2- ALKYL(ARYL)]SULFONYLBENZENE-SULFONYL CHLORIDES AND THEIR INTERMEDIATES
    7.
    发明公开
    PROCESS FOR THE PREPARATION OF 2- ALKYL(ARYL)]SULFONYLBENZENE-SULFONYL CHLORIDES AND THEIR INTERMEDIATES 审中-公开
    HERSTELUNG方法2-¬ALKYL（芳基）SULFONYLBENZOL磺酰基及中间体

    公开(公告)号：EP1442012A1

    公开(公告)日：2004-08-04

    申请号：EP02776391.1

    申请日：2002-10-31

    申请人： Wyeth

    发明人： KRISHNAN, Lalitha ,  WILK, Bogdan, Kazimierz ,  VARRIANO, Jennifer, Patricia

    IPC分类号： C07C315/00 ,  C07C317/14 ,  C07C315/04 ,  C07C317/36

    CPC分类号： C07C315/00 ,  C07C315/04 ,  C07C317/14 ,  C07C317/36

    摘要： A process for the preparation of 2-[alkyl(aryl)]sulfonylbenzene sulfonyl chlorides of the formula (I), in which R is alkyl or aryl substituted at the ortho or meta positions with alkyl, aryl, NHAc or alkoxy, comprising the steps of: a) reacting 2-chloronitrobenzene, 2-fluoronitrobenzene or 2-bromonitrobenzene with a compound of the following formula: RSO2-M+ wherein R is defined above; and M is sodium, potassium, lithium, ammonium or quaternary ammonium, in a polar aprotic solvent at a temperature of about 50 to 190°C; b) reacting the material prepared in step (a) with hydrogen at a pressure of about 20 to about 60 psi in a polar aprotic solvent at a temperature of about 20 to about 60°C; and c) diazotizing the material prepared in step (b) with sodium nitrite in the presence of hydrochloric acid and reacting the resulting diazonium salt with sulfur dioxide in the presence of copper (I) or copper (II) compounds or a mixture thereof, in water.

    Benzosulfone derivatives
    10.
    发明公开
    Benzosulfone derivatives 有权
    Benzosulfonderivate

    公开(公告)号：EP0930302A2

    公开(公告)日：1999-07-21

    申请号：EP99100149.6

    申请日：1999-01-08

    申请人： F.HOFFMANN-LA ROCHE AG

    发明人： Bös, Michael ,  Hunkeler, Walter ,  Riemer, Claus

    IPC分类号： C07D239/38 ,  C07D213/71 ,  C07D213/74 ,  C07D213/73 ,  C07C317/36 ,  C07D213/84 ,  A61K31/505

    CPC分类号： C07D213/73 ,  C07C317/36 ,  C07D213/71 ,  C07D213/74 ,  C07D213/84 ,  C07D239/38

    摘要： The present invention relates to novel compounds of the general formula
    wherein

    R 1 is hydrogen;
    R 2 is hydrogen, trifluoromethyl or lower alkyl;
    R 3 is hydrogen or amino; or
    R 1 and R 2 or R 3 and R 2 taken together are -CH=CH-CH=CH-;
    Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl;
    R 4, R 5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C 3 -C 6 cycloalkyl, C 3 -C 6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group -NH(CH 2 ) n NR 6 R 7 , -N(CH 3 )(CH 2 ) n NR 6 R 7 , -NH(CH 2 ) n -morpholin-4-yl or -NH(CH 2 ) n OH;
    n is 2-4
    R 6 and R 7 are each independently hydrogen or lower alkyl,
    and to their pharmaceutically acceptable salts.

    It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.

    摘要翻译： 本发明涉及通式的新化合物，其中R 1是氢; R 2是氢，三氟甲基或低级烷基; R 3是氢或氨基; 或R 1和R 2或R 3和R 2一起是-CH = CH-CH = CH-; Z是嘧啶-4-基，吡啶-4-基，吡啶-2-基或苯基; R 4，R 5各自独立地为氢，低级烷基，三氟甲基，卤素，低级烷氧基，次氮基，氨基，低级烷基 - 氨基，二低级烷基 - 氨基，哌嗪基，吗啉基，吡咯烷基，乙烯基， C 6环烷基，C 3 -C 6环烯基，叔丁基乙酰基，羟基烷基乙烯基，苯乙酰基，萘基，噻吩基或苯基，其可以被卤素，低级烷氧基，低级烷基，三氟甲基或硝基取代，或基团-NH（CH 2）n NR （CH 3）（CH 2）n NR 6 R 7，-NH（CH 2）n - 吗啉-4-基或-NH（CH 2）n OH; n是2-4 R 6和R 7各自独立地是氢或低级烷基，以及它们的药学上可接受的盐。 已经发现，式I化合物对5HT-6受体具有选择性亲和力。