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    METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES
    2.
    发明申请
    METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES 审中-公开
    二硫青霉烯类化合物和中间体的制备方法

    公开(公告)号：WO2005123701A1

    公开(公告)日：2005-12-29

    申请号：PCT/IB2005/001874

    申请日：2005-06-03

    申请人： PHARMACIA CORPORATION? ,  LETENDRE, Leo, J. ,  SNODDY, Cynthia, K. ,  KLEMM, George, H. ,  LAWSON, Jon, P. ,  BAUER, Michael, J.

    发明人： LETENDRE, Leo, J. ,  SNODDY, Cynthia, K. ,  KLEMM, George, H. ,  LAWSON, Jon, P. ,  BAUER, Michael, J.

    IPC分类号： C07D261/04

    CPC分类号： C07D261/04 ,  C07D261/08

    摘要： The disclosure provides a method for the preparation of a diarylisoxazolé sulfonamide compound comprising contacting a deoxybenzoin with a secondary amine to form a diarylenamine compound; contacting the diarylenamine compound with an acetylating agent to form an acetyl diarylenamine compound; contacting the acetyl diarylenamine compound with a source of hydroxylamine to form an diaryl isoxazolol compound; eliminating water from the diaryl isoxazolol compound to form a diaryl isoxazole compound, chlorosulfonating the diarylisoxazole compound to form a chlorosulfonyl diaryl isoxazole compound; and contacting the chlorosulfonyl diaryl isoxazole compound with a source of ammonia to form the diarylisoxazole sulfonamide compound.

    摘要翻译： 本公开提供了制备二芳基异恶唑磺酰胺化合物的方法，包括使脱氧苯偶姻与仲胺接触以形成二芳基胺化合物; 使二芳基胺化合物与乙酰化剂接触以形成乙酰基二芳基胺化合物; 使乙酰二芳基胺化合物与羟胺源接触形成二芳基异恶唑烷化合物; 从二芳基异恶唑醇化合物中除去水，形成二芳基异恶唑化合物，氯化二芳基异恶唑化合物，形成氯磺酰基二芳基异恶唑化合物; 并将氯磺酰基二芳基异恶唑化合物与氨源接触以形成二芳基异恶唑磺酰胺化合物。

    PROCESSES FOR PREPARATION OF 9,11-EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN
    4.
    发明申请
    PROCESSES FOR PREPARATION OF 9,11-EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN 审中-公开
    制备9,11-环氧甾体和中间体有用的方法

    公开(公告)号：WO1998025948A2

    公开(公告)日：1998-06-18

    申请号：PCT/US1997023090

    申请日：1997-12-11

    申请人： G.D. SEARLE & CO. ,  NG, John, S. ,  LIU, Chin ,  ANDERSON, Dennis, K. ,  LAWSON, Jon, P. ,  WIECZOREK, Joseph ,  KUNDA, Sastry, A. ,  LETENDRE, Leo, J. ,  POZZO, Mark, J. ,  SING, Yuen-Lung, L. ,  WANG, Ping, T. ,  YONAN, Edward, E. ,  WEIER, Richard, M. ,  KOWAR, Thomas, R. ,  BAEZ, Julio, A. ,  ERB, Bernhard

    发明人： G.D. SEARLE & CO.

    IPC分类号： C07J00/00

    CPC分类号： C12P33/10 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J53/002 ,  C07J71/0005 ,  C07J71/0015 ,  C12P33/005

    摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of formula (I) wherein: -A-A- represents the group -CHR -CHR - or -CR =CR -, R , R and R are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy; R represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; -B-B- represents the group -CHR -CHR - or an alpha- or beta-oriented group (III), where R and R are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R and R are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R and R together comprise a carbocyclic or heterocyclic ring structure, or R or R together with R or R comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

    摘要翻译： 提供了多种新的反应方案，新的方法步骤和新的中间体，用于合成环氧基异丙肾上腺素和其它式（I）化合物，其中：-AA-表示基团-CHR 4 -CHR 5 - 或-CR 4 = CR 5 - ，R 3，R 4和R 5独立地选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基， 芳; R 1表示α-取代的低级烷氧基羰基或羟烷基; -BB-代表基团-CHR 6 -CHR 7 - 或α或β-取代基团（III），其中R 6和R 7独立地选自氢， 卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基; R 8和R 9独立地选自氢，羟基，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基，或R 8。 并且R 9一起包含碳环或杂环结构，或R 8或R 9与R 6或R 7一起包含与五环D环稠合的碳环或杂环结构。