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1. 发明申请

WO2006032970A2 PROCESS FOR PREPARING 7a-ALKOXYCARBONYL SUBSTITUTED STEROIDS 审中-公开
标题翻译：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。

2. 发明申请

WO2005092913A1 IMPROVED PROCESS FOR THE PREPARATION OF 9,11 EPOXY STEROIDS 审中-公开
标题翻译：改进制备9,11环氧甾体的方法
公开(公告)号：WO2005092913A1
公开(公告)日：2005-10-06
申请号：PCT/US2005/009381
申请日：2005-03-22
申请人： PHARMACIA & UPJOHN COMPANY , WIECZOREK, Joseph, J. , MAISTO, Keith, D. , DAVID, Paul , CARLOS, Marlon, V. , KIM, Chung, C.
发明人： WIECZOREK, Joseph, J. , MAISTO, Keith, D. , DAVID, Paul , CARLOS, Marlon, V. , KIM, Chung, C.
IPC分类号： C07J71/00
CPC分类号： C07J21/00 , C07J71/00 , Y02P20/582
摘要： Processes are described for epoxidation reactions. In particular, the process comprises the conversion of a steroid substrate having an olefinic unsaturation in the steroid nucleus to a structure comprising a 9,11-epoxy substituent by reaction of the substrate with a peroxide compound in the presence of a peroxide activator. The epoxidation processes described are conducted at relatively low hydrogen peroxide to steroid substrate ratio. Several optional process modifications are described.
摘要翻译：描述了用于环氧化反应的方法。特别地，该方法包括通过在过氧化物活化剂存在下使底物与过氧化物反应，将类固醇核中具有烯属不饱和键的类固醇底物转化成包含9,11-环氧取代基的结构。所描述的环氧化方法在相对低的过氧化氢条件下进行至类固醇底物的比例。描述了几个可选的过程修改。

3. 发明申请

WO2006032970A3 PROCESS FOR PREPARING 7α-ALKOXYCARBONYL SUBSTITUTED STEROIDS 审中-公开
公开(公告)号：WO2006032970A3
公开(公告)日：2006-03-30
申请号：PCT/IB2005/002757
申请日：2005-08-25
申请人： PHARMACIA CORPORATION , 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
摘要： Processes are described for the conversion of a steroid substrate having a 4,7-carbonyl bridge to a structure comprising a 7α-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 7α-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 7α-alkoxycarbonyl substituted steroid product. Alternatively, the repulp solution may be recycled to a primary reactor wherein 4,7-carbonyl bridge substrate is converted to 7α-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 11α-hydroxy-7α-methoxycarbonyl compound (hydroxyester), the 11α-hydroxy group is converted to a leaving group which is then abstracted to produce a Δ-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.

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