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    PROCESS FOR PREPARING 7a-ALKOXYCARBONYL SUBSTITUTED STEROIDS
    1.
    发明申请
    PROCESS FOR PREPARING 7a-ALKOXYCARBONYL SUBSTITUTED STEROIDS 审中-公开
    制备7a-烷氧基羰基取代的类固醇的方法

    公开(公告)号：WO2006032970A2

    公开(公告)日：2006-03-30

    申请号：PCT/IB2005002757

    申请日：2005-08-25

    申请人： PHARMACIA CORP ,  ABBAS S ZAHEER ,  BAUER MICHAEL ,  CARLOS MARLON V ,  DAVID PAUL ,  FRANCZYK THADDEUS ,  KIM CHUNG C ,  LAWSON JON P ,  MAISTO KEITH D ,  MCKENZIE DAVID ,  POZZO MARK ,  WIECZOREK JOSEPH

    发明人： ABBAS S ZAHEER ,  BAUER MICHAEL ,  CARLOS MARLON V ,  DAVID PAUL ,  FRANCZYK THADDEUS ,  KIM CHUNG C ,  LAWSON JON P ,  MAISTO KEITH D ,  MCKENZIE DAVID ,  POZZO MARK ,  WIECZOREK JOSEPH

    IPC分类号： C07J53/00 ,  C07J21/00

    CPC分类号： C07J21/001 ,  C07J53/002 ,  Y02P20/582

    摘要： Processes are described for the conversion of a steroid substrate having a 4,7-carbonyl bridge to a structure comprising a 7a-alkoxycarbonyl substituent by reaction of the substrate with an alkoxy group source, preferably in the presence of a base. Several optional process modifications are described. The reaction may be conducted at a temperature greater than about 70°C, with substantially shorter residence times than are required at lower temperatures. A saponification target may be incorporated into the reaction medium to consume free hydroxide compounds. The product 7a-alkoxycarbonyl compound may be recovered by crystallization, residual steroid values may be recovered from the crystallization mother liquor by extraction, and the extract may be processed to produce a repulp solution wherein the steroids may be re-equilibrated to produce additional 7a-alkoxycarbonyl substituted steroid product. Alternatively, the repulp solution may be recycled to a primary reactor wherein 4,7-carbonyl bridge substrate is converted to 7a-alkoxycarbonyl product. The process is particularly useful in the preparation of eplerenone, wherein a diketone intermediate comprising a 4,7-carbonyl bridge is reacted with an alkali metal methoxide to yield an 11a-hydroxy-7a-methoxycarbonyl compound (hydroxyester), the 11a-hydroxy group is converted to a leaving group which is then abstracted to produce a ?-9,11 enester, and the enester is epoxidized to eplerenone. Also disclosed is an epoxidation reaction conducted at relatively low hydrogen peroxide to enester substrate ratio.

    摘要翻译： 描述了通过底物与烷氧基源优选在碱存在下反应将具有4,7-羰基桥的类固醇底物转化为包含7α-烷氧基羰基取代基的结构的方法。 描述了几个可选的过程修改。 该反应可以在大于约70℃的温度下进行，其停留时间明显短于在较低温度下所需的停留时间。 可以将皂化目标结合到反应介质中以消耗游离的氢氧化物化合物。 产物7a-烷氧基羰基化合物可以通过结晶回收，可以通过萃取从结晶母液中回收剩余的类固醇值，并且可以对提取物进行处理以产生再溶解溶液，其中类固醇可以被再平衡以产生另外的7a- 烷氧羰基取代的甾体产物。 或者，再浆化溶液可循环至其中4,7-羰基桥基质被转化为7α-烷氧基羰基产物的主反应器。 该方法在制备依普利农中特别有用，其中使包含4,7-羰基桥的二酮中间体与碱金属甲醇盐反应，得到11a-羟基-7a-甲氧基羰基化合物（羟基酯），11a-羟基 转化为离去基团，然后将其抽出以产生α-9,11烯烃，并将烯烃环氧化成依普利农。 还公开了在相对较低的过氧化氢与烯烃底物比例下进行的环氧化反应。

    PROCESSES FOR PREPARATION OF 9,11-EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN
    6.
    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。

    METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES
    7.
    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。