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1. 发明申请

WO9825948A3 PROCESSES FOR PREPARATION OF 9,11-EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN 审中-公开
标题翻译：制备9,11-环氧甾体和中间体有用的方法
公开(公告)号：WO9825948A3
公开(公告)日：1998-10-15
申请号：PCT/US9723090
申请日：1997-12-11
申请人： 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： 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
IPC分类号： C07D301/12 , C07J1/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J53/00 , C07J71/00 , C12P33/00 , C12P33/10 , C07J
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 -CHR4-CHR5- or -CR?4=CR5-, R3, R4 and R5¿ are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy; R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; -B-B- represents the group -CHR6-CHR7- or an alpha- or beta-oriented group (III), where R?6 and R7¿ are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R?8 and R9¿ 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?8 and R9¿ together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 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，新工艺步骤和新的中间体，用于合成环氧麦芽糖酮和式I的其它化合物，其中AA-代表基团-CHR4-CHR5-或-CR4 = CR5-; R3，R4和R5独立地选自卤代，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基和芳氧基; R1代表α-取代的低级烷氧基羰基或羟基烷基; -BB-代表基团-CHR6-CHR7- 或α-取代或β-取代基团：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，烷氧基羰基烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基，或R8和R9一起包含碳环或杂环结构，或R 8或R 9与R 6一起或包含与五环D环稠合的碳环或杂环结构。

2. 发明申请

WO0168637A3 METHOD FOR THE PREPARATION OF TETRAHYDROBENZOTHIEPINES 审中-公开
标题翻译：制备四氢生物素的方法
公开(公告)号：WO0168637A3
公开(公告)日：2003-01-09
申请号：PCT/US0107421
申请日：2001-03-08
申请人： PHARMACIA CORP , BABIAK KEVIN A , CARPENTER ANDREW , CHOU SHINE , COLSON PIERRE-JEAN , FARID PAYMAN , HETT ROBERT , HUBER CHRISISTIAN H , KOELLER KEVIN J , LAWSON JON P , LI JAMES , MAR EDUARDO K , MILLER LAWRENCE M , ORLOVSKI VLADISLAV , PETERSON JAMES C , POZZO MARK J , PRZYBYLA CLAIRE A , TREMONT SAMUEL J , TRIVEDI JAY S , WAGNER GRACE M , WEISENBURGER GERALD A , ZHI BENXIN
发明人： BABIAK KEVIN A , CARPENTER ANDREW , CHOU SHINE , COLSON PIERRE-JEAN , FARID PAYMAN , HETT ROBERT , HUBER CHRISISTIAN H , KOELLER KEVIN J , LAWSON JON P , LI JAMES , MAR EDUARDO K , MILLER LAWRENCE M , ORLOVSKI VLADISLAV , PETERSON JAMES C , POZZO MARK J , PRZYBYLA CLAIRE A , TREMONT SAMUEL J , TRIVEDI JAY S , WAGNER GRACE M , WEISENBURGER GERALD A , ZHI BENXIN
IPC分类号： C07D317/18 , A61K31/235 , A61K31/38 , A61K31/495 , A61K31/4995 , A61P3/06 , A61P43/00 , C07B53/00 , C07B55/00 , C07B57/00 , C07B61/00 , C07C201/12 , C07C205/35 , C07C315/02 , C07C315/04 , C07C317/24 , C07C317/36 , C07C319/14 , C07C321/28 , C07D337/08 , C07D409/12 , C07D487/08 , C07C31/36 , C07C45/29 , C07C47/14 , C07C69/63 , C07D317/24 , C07D317/36
CPC分类号： C07D409/12 , A61K31/235 , A61K31/38 , A61K31/495 , C07D337/08 , C07D487/08 , A61K2300/00
摘要： Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.
摘要翻译：在其几个实施方案中，本发明提供了一种制备四氢苯并噻吩一-1,1-二氧化物化合物的改进方法; 提供了由这种化合物的单一非对映异构体制备四氢苯并噻吩一-1,1-二氧化物化合物的非对映体混合物的方法; 提供了制备3-溴-2-取代的丙醛化合物的方法; 并提供了制备3-硫代-2-取代的丙醛化合物的方法。

3. 发明申请

WO2004087074A3 PROCESS FOR MAKING SUBSTITUTED PYRAZOLES 审中-公开
标题翻译：制备取代的吡唑的方法
公开(公告)号：WO2004087074A3
公开(公告)日：2005-03-24
申请号：PCT/US2004009659
申请日：2004-03-30
申请人： PHARMACIA CORP , ALLEN KIMBERLEY C , ANDERSON DENNIS K , BALDUS JOHN E , BOEHLOW TODD , CLARK JERRY D , DUKESHERER DANIEL R , EDNEY ALBERT D , FEVIG TOM , KUNDA SASTRY , LAWSON JON P , LAU PATRICK H , MCDERMOTT LISA L , MAO MICHAEL K , MOE JODI L , MUDIPALLI PARTHA , NAING WIN , SELNESS SHAUN R , SEYMOUR CHRISTINE B , SCHILKE TOBIN C , VISWANATH SHEKHAR , WALKER JOHN K , YALAMANCHILI GOPICHAND
发明人： ALLEN KIMBERLEY C , ANDERSON DENNIS K , BALDUS JOHN E , BOEHLOW TODD , CLARK JERRY D , DUKESHERER DANIEL R , EDNEY ALBERT D , FEVIG TOM , KUNDA SASTRY , LAWSON JON P , LAU PATRICK H , MCDERMOTT LISA L , MAO MICHAEL K , MOE JODI L , MUDIPALLI PARTHA , NAING WIN , SELNESS SHAUN R , SEYMOUR CHRISTINE B , SCHILKE TOBIN C , VISWANATH SHEKHAR , WALKER JOHN K , YALAMANCHILI GOPICHAND
IPC分类号： A61K20060101 , A61P29/00 , C07D211/36 , C07D401/04 , C07D401/06 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： This invention is directed generally to a process for making substituted pyrazoles, tautomers of the substituted pyrazoles, and salts of the substituted pyrazoles and tautomers. The substituted pyrazoles correspond in structure to Formula (I) wherein R R R , Y , Y , Y , Y , and Y are as defined in the specification.
摘要翻译：本发明一般涉及制备取代的吡唑，取代的吡唑的互变异构体和取代的吡唑和互变异构体的盐的方法。取代的吡唑在结构上对应于其中R 3A，R 3B，Y 1，Y 2，Y 3，Y 4和Y 5中的式（I）如说明书中所定义。

4. 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。

5. 发明申请

WO9721720A3 Processes for preparation of 7 alpha-carboxyl 9,11-epoxy steroids and intermediates useful therein and a general process for the epoxidation of olifinic double bonds 审中-公开
标题翻译：用于制备7αα-羧基9,11-环氧类固醇和其中有用的中间体的方法和用于环氧化奥利膦酸双键的通用方法
公开(公告)号：WO9721720A3
公开(公告)日：1997-10-30
申请号：PCT/US9620780
申请日：1996-12-11
申请人： SEARLE & CO
发明人： NG JOHN S , WANG PING T , BAEZ JULIO A , LIU CHIN , ANDERSON DENNIS K , LAWSON JON P , WIECZOREK JOSEPH , MUCCIARIELLO GENNARO , VANZANELLA FORTUNATO , KUNDA SASTRY A , LETENDRE LEO J , POZZO MARK J , SING YUEN-LUNG L
IPC分类号： A61K31/58 , C07J19/00 , C07J21/00 , C07J31/00 , C07J53/00 , C07J71/00 , C12P33/00 , C12P33/10 , C12Q1/02
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
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-, -B-B-, R 1 , R 3 , R 8 and R 9 are as defined in the specification.
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，用于合成环氧麦克风和其它式I化合物，其中：-AA-，-BB-，R 1，R 3， / SUP>，R 8和R 9如说明书中所定义。

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