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    Carbacyclins, processes for their preparation, and their use as medicinal agents
    1.
    发明授权
    Carbacyclins, processes for their preparation, and their use as medicinal agents 失效

    公开(公告)号：US5162353A

    公开(公告)日：1992-11-10

    申请号：US570446

    申请日：1990-08-21

    申请人： Helmut Vorbrueggen ,  Bob Nieuweboer ,  Claus-Steffen Stuerzebecher

    发明人： Helmut Vorbrueggen ,  Bob Nieuweboer ,  Claus-Steffen Stuerzebecher

    IPC分类号： C07C59/62 ,  C07C405/00

    CPC分类号： C07C59/62 ,  C07C405/0083

    摘要： The invention relates to carbacyclin derivatives with general formula I: ##STR1## in which Y.sub.1 stands for the radical --CH.sub.2 --X--(CH.sub.2).sub.n --R.sub.1 or the radical ##STR2## n, 1 or 3, R.sub.1, the radical ##STR3## the radical ##STR4## R.sub.9 stands for the radical --(CH.sub.2).sub.m --R.sub.6 or the radical --(CH.sub.2).sub.m-o --[Z.sub.1 --(CH.sub.2).sub.m-p ].sub.x --[Z.sub.2 --(CH.sub.2).sub.m-q ].sub.y --R.sub.6,m=2-20,o, p, and q are less than or equal to 19,x, y=0, 1 or 2,Z.sub.1 stands for a cis--CH.dbd.CH group, a trans--CH.dbd.CH group of a --C.dbd.C group, and each of these groups must be separated at least by a methylene group from the C-9 carbon atom of the carbacyclin bicyclic compound,Z.sub.2 stands for oxygen, sulfur, an NH or an N methyl group,R.sub.6 stands for amino, methylamino, hydroxy, carboxy or mercapto,X an oxygen atom or a methylene group,Y.sub.2 hydrogen or fluorine,A a --CH.sub.2 --CH.sub.2, trans--CH.dbd.CH or --C.dbd.C group,W a free or functionally modified hydroxy methylene group,D a straight-chain, saturated alkylene group with 1-5 C atoms,E stands for a direct bond, a --C.tbd.C group or a --CH.dbd.CR.sub.7 group,R.sub.4 stands for an alkyl group with 1-10 C atoms,R.sub.5 stands for a free or functionally modified hydroxy group.The invention also relates to carbacyclin derivatives of general Formula I' ##STR5## wherein n is 1 or 3R.sub.1 is the residue ##STR6## the residue ##STR7## the residue COOR.sub.2 wherein R.sub.2 can mean hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue, or is the residue CONHR.sub.3 with R.sub.3 meaning hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.tbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydrogen, hydroxy, amino or trimethylsilyl,X is an oxygen atom or, if R.sub.9 means an alkyl group of 5-10 carbon atoms, a methylene group, andY is hydrogen or fluorine, to processes for their preparation, and to medicinal agents containing these compounds.

    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents
    2.
    发明授权
    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents 失效
    3-OXA-5-FLOORO-CARBACYCLINS，其制备和用作药物代理

    公开(公告)号：US5157042A

    公开(公告)日：1992-10-20

    申请号：US713002

    申请日：1991-06-10

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    IPC分类号： C07C69/708 ,  A61K31/225 ,  A61K31/35 ,  A61K31/351 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  C07C51/00 ,  C07C51/367 ,  C07C59/125 ,  C07C59/62 ,  C07C67/00 ,  C07C67/31 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/88 ,  C07C405/00 ,  C07D309/12 ,  C07D317/72

    CPC分类号： C07D317/72 ,  C07C405/0083

    摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2 ;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms; or a branched, saturated or straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms; all of which are substituted by fluorine atoms;n is 1, 2, or 3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.7 is hydrogen, halogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group; andR.sub.5 is a free or functionally modified hydroxy group; andwhen R.sub.1 is OH, the salts thereof with physiologically compatible bases,are valuable pharmacological agents.

    摘要翻译： 式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，烷基，环烷基，芳基，杂芳基或杂环残基; 或R1是NHR3，其中R3是酸残基（酰基）或R2; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH基可以是α-或β-位; D是1-10个碳原子的直链饱和脂族基团; 或2-10个碳原子的支链，饱和或直链或支链的不饱和脂族基团; 所有这些都被氟原子取代; n为1,2或3; E是直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6是氢或1-5个碳原子的烷基，R 7是氢，卤素或1-5个碳原子的烷基; R4是脂族基团，环烷基，任选取代的芳基或杂环基; R5是游离或官能改性的羟基; 当R1是OH时，其与生理上相容的碱的盐是有价值的药剂。

    Novel carbacyclins, processes for their production and their use as medicinal agents
    4.
    发明授权
    Novel carbacyclins, processes for their production and their use as medicinal agents 失效
    新型碳霉素，其生产工艺及其作为药剂的使用

    公开(公告)号：US4827017A

    公开(公告)日：1989-05-02

    申请号：US21102

    申请日：1987-03-03

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Ekkehard Schillinger ,  Claus-Steffen Stuerzebecher

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Ekkehard Schillinger ,  Claus-Steffen Stuerzebecher

    IPC分类号： C07D309/12 ,  A61K31/557 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C45/00 ,  C07C49/835 ,  C07C51/00 ,  C07C65/19 ,  C07C67/00 ,  C07C69/76 ,  C07C69/773 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/0083

    摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2 wherein R.sub.2 is hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.6 -C.sub.10 -aryl, ##STR2## or a heterocyclic residue, or R.sub.1 is R.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.6 -C.sub.10 -aryl, C.sub.7 -C.sub.14 -aralkyl or a heterocyclic residue,A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated alkylene group of 1-10 carbon atoms, or a branched, saturated or a straight-chain or branched, unsaturated alkylene group of 2-10 carbon atoms, each of which can optionally by substituted by fluorine atoms,n is the number 1, 2 or 3,E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and one is hydrogen and the other alkyl of 1-5 carbon atoms, or one is hydrogen and the other is halogen, orE can also be --CH.sub.2 CH.sub.2 -- when R.sub.1 is R.sub.3,R.sub.4 is C.sub.1-10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, optionally substituted C.sub.6 -C.sub.10 -aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy group and, when R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases;are useful as medicinal agents.

    摘要翻译： 式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基，或者杂环残基，或者R 1是R 3 其中R 3是C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基，C 7 -C 14 - 芳烷基或杂环残基，A是-CH 2 -CH 2 - ，反式-CH = CH-或-C - ，W是游离或官能改性的羟基亚甲基或游离的或功能上被修饰的“IMAGE”，其中OH基可以是α或β-位，D是直链，饱和的亚烷基 1-10个碳原子，或2-10个碳原子的支链，饱和或直链或支链不饱和的亚烷基，其各自可任选被氟原子取代，n为数1,2或3， E是-C 3位C或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，一个是氢，1-5个碳原子的另一个烷基，或一个是氢，另一个是卤素，或者也可以是 当R 1为R 3，R 4为C 1-10时为-CH 2 CH 2 - 烷基，C 3 -C 10 - 环烷基，任选取代的C 6 -C 10 - 芳基或杂环基，R 5是游离或官能改性的羟基，并且当R 2是氢时，其与生理上相容的碱的盐; 作为药剂有用。

    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents
    5.
    发明授权
    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents 失效
    9-氟前列腺素衍生物，其制备和用作药物

    公开(公告)号：US4789685A

    公开(公告)日：1988-12-06

    申请号：US4733

    申请日：1987-01-20

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0041

    摘要： 9-fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, the physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.

    摘要翻译： 其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的α-氟仿烷基衍生物。 或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α或β位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚链烯基 可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选被取代的芳基或杂环基，当R2是H时，生理上相容的盐 具有有价值的药理学性质，例如作为骨质疏松症或流产者。

    Novel carbacyclinamides, their preparation and use as medicinal agents
    6.
    发明授权
    Novel carbacyclinamides, their preparation and use as medicinal agents 失效
    新型卡巴胆碱，其制备和用作药物

    公开(公告)号：US4552875A

    公开(公告)日：1985-11-12

    申请号：US510125

    申请日：1983-07-01

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael H. Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael H. Town

    IPC分类号： A61K31/16 ,  A61K31/19 ,  A61K31/535 ,  A61K31/5375 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/10 ,  C07C231/12 ,  C07C233/21 ,  C07C235/06 ,  C07C235/08 ,  C07C235/14 ,  C07C235/16 ,  C07C235/30 ,  C07C405/00 ,  C07D295/18 ,  C07H13/04 ,  C07C177/00 ,  A61K31/557

    CPC分类号： C07H13/04 ,  C07C405/0083

    摘要： Carbacyclinamides of Formula I ##STR1## wherein R.sub.1 is NHR.sub.4, wherein R.sub.4 is H, --(CH.sub.2).sub.n --R.sub.8 or straight-chained or branched aliphatic groups of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 each are straight-chained or branched, lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.4 and R.sub.5 together with the adjoining N-atom form a 5- or 6-membered heterocycle which can optionally contain additional hetero atoms and can be substituted; or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 is an aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, and R.sub.5 is straight-chained or branched aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms;n is 1-4;R.sub.8 is --CONH.sub.2 or --N(C.sub.1 -C.sub.4 -alkyl).sub.2 ;R.sub.2 is a free or functionally modified hydroxy group;R.sub.3 is aliphatic, cycloalkyl, optionally substituted aryl, or a heterocyclic group;X is oxygen or --CH.sub.2 --;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --CH.tbd.--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR3## a straight-chain, saturated aliphatic group of 1-5 carbon atoms, or a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-5 carbon atoms, all of which groups can optionally be substituted by fluorine atoms;m is 1-3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --wherein R.sub.6 and R.sub.7 are each a hydrogen atom or an alkyl group of 1-5 carbon atomshave valuable pharmacological properties.

    摘要翻译： 式I的卡拉菌素酰胺其中R 1是NHR 4，其中R 4是H， - （CH 2）n -R 8或1-10个碳原子的直链或支链脂族基团，3-10个碳原子的环烷基， 芳基或2-8个碳原子的低级单 - 或多羟基烷基，或R1是NR4R5，其中R4和R5各自是2-8个碳原子的直链或支链，低级，单 - 或多羟基烷基，或R4和R5连同 邻接的N-原子形成5-或6-元杂环，其可以任选地含有另外的杂原子并且可以被取代; 或R1是NR4R5，其中R4是1-10个碳原子的脂族基团，3-10个碳原子的环烷基，R5是1-10个碳原子的直链或支链脂族基团，3-10个碳原子的环烷基， 芳基或更低级的2-8个碳原子的单或多羟基烷基; n为1-4; R8是-CONH2或-N（C1-C4-烷基）2; R2是游离或官能改性的羟基; R3是脂族，环烷基，任选取代的芳基或杂环基; X是氧或-CH 2 - ; A是-CH 2 -CH 2 - ，反式-CH = CH-或-CH 3 OCH 3 - 。 W是游离的或官能改性的羟基亚甲基或游离或功能改性的“IMAGE”，其中OH-基团可以是α-或β-位; D是1-5个碳原子的直链饱和脂族基团，或2-5个碳原子的支链，饱和或直链或支链不饱和脂肪族基团，所有这些基团可任选地为 被氟原子取代; m为1-3; E是直接键，-C 3 D或-CR 6 = CR 7 - 其中R 6和R 7各自为氢原子或1-5个碳原子的烷基具有有价值的药理学性质。

    9-Bromoprostaglandins, their preparation, and their use as medicaments
    7.
    发明授权
    9-Bromoprostaglandins, their preparation, and their use as medicaments 失效
    9-溴前列​​腺素，其制剂及其用作药物

    公开(公告)号：US4487953A

    公开(公告)日：1984-12-11

    申请号：US446888

    申请日：1982-12-06

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger

    IPC分类号： A61K31/16 ,  A61K31/19 ,  A61K31/20 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D309/12 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0041

    摘要： Compounds of Formula (I) ##STR1## wherein the 9-bromine atom can be in the .alpha.- or .beta.-position,R.sub.1 is CH.sub.2 OH or C(O)OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is C(O)NHR.sub.3 wherein R.sub.3 is an acid residue or R.sub.2 ; andA is --CH.sub.2 --CH.sub.2 -- or cis --CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 --, trans --CH.dbd.CH--, or --C.tbd.C--;W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D and E together are a direct bond; orD is straight-chain, branched, or cyclic alkylene of 1-10 carbon atoms, optionally substituted by fluorine atoms; andE is oxygen, sulfur, a direct bond --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 and R.sub.7 are different from each other and each is hydrogen, chlorine, or C.sub.1 -C.sub.4 -alkyl;R.sub.4 is a free or functionally modified hydroxy group;R.sub.5 is hydrogen, alkyl, halo-substituted alkyl, cycloalkyl, optionally substituted aryl, or a heterocyclic group; and, when R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases,are pharmacologically active compounds, e.g., as abortifacients.

    摘要翻译： 式（I）化合物其中9-溴原子可以是α或β-位，R1是CH2OH或C（O）OR2，其中R2是氢，烷基，环烷基，芳基， 或杂环残基; 或R 1为C（O）NHR 3，其中R 3为酸残基或R 2; 并且A是-CH 2 -CH 2 - 或顺式-CH = CH-; B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH基可以是α-或β-位; D和E一起是直接的债券; 或D是1-10个碳原子的直链，支链或环状亚烷基，任选被氟原子取代; 并且E是氧，硫，直接键-C 3或C 6或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或C 1 -C 4 - 烷基; R4是游离的或官能改性的羟基; R5是氢，烷基，卤素取代的烷基，环烷基，任选取代的芳基或杂环基; 并且当R 2为氢时，其与生理上相容的碱的盐是药理活性化合物，例如作为流产者。

    Process for the preparation of oxaprostaglandin intermediates
    8.
    发明授权
    Process for the preparation of oxaprostaglandin intermediates 失效
    制备奥沙星胃酸中间体的方法

    公开(公告)号：US4191823A

    公开(公告)日：1980-03-04

    申请号：US856544

    申请日：1977-12-01

    申请人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbrueggen

    发明人： Werner Skuballa ,  Bernd Raduchel ,  Helmut Vorbrueggen

    IPC分类号： C07D307/935 ,  C07F9/40 ,  C07D307/83

    CPC分类号： C07D307/935 ,  C07F9/4006

    摘要： In a process for the preparation of an oxaprostaglandin intermediate of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, or a free or functionally modified hydroxy group;R.sub.2 and R.sub.3 are the same or different, and each is hydrogen, halogen or alkyl;R.sub.4 is alkyl or optionally substituted aryl; andn is 0, 1, 2 or 3;which comprises reacting an aldehyde of the formula ##STR2## wherein R.sub.1 is as defined above with an anion of the formula ##STR3## wherein n, R.sub.2, R.sub.3 and R.sub.4 are as defined above; andR.sub.5 is alkyl;an improvement is provided wherein the anion is added to the reaction medium in a form which consists essentially of its crystalline alkali metal salt of the formula ##STR4## wherein A is an alkali metal atom.

    摘要翻译： 在制备下式的“草药前列腺素中间体”的方法中，其中R 1是氢，烷基或游离或官能改性的羟基; R2和R3相同或不同，各自为氢，卤素或烷基; R4是烷基或任选取代的芳基; 并且n为0,1,2或3; 其包括使式IMA的醛与其中R1如上所定义的式与下式的阴离子反应，其中n，R 2，R 3和R 4如上定义; R5是烷基; 提供了一种改进，其中阴离子以基本上由其结构式为下式的碱金属盐组成的形式加入到反应介质中，其中A是碱金属原子。

    Pharmaceutically active 9-chloroprostaglandins
    10.
    发明授权
    Pharmaceutically active 9-chloroprostaglandins 失效
    药用活性9-氯前列腺素

    公开(公告)号：US5204371A

    公开(公告)日：1993-04-20

    申请号：US792574

    申请日：1991-11-15

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Ekkehard Schillinger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Ekkehard Schillinger

    IPC分类号： C07C405/00

    CPC分类号： C07C405/0041 ,  C07C405/00

    摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.-or .beta.-position,A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2,--, trans--CH.dbd.CH--, or --CH.tbd.C--, W is hydroxymethylene orD and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacologoical properties.

    摘要翻译： 其中9-氯原子可以是α-或β-位的式为“IMAGE”的化合物，A为-CH 2 -CH 2 - 或顺式-CH = CH-，B为-CH 2 -CH 2， - ， CH = CH-或-CH 3 B - ，W是羟基亚甲基或D和E一起代表直接键，或D是1-10个碳原子的直链或支链亚烷基，任选被氟取代，E是 氧或硫或直接键，并且R4是如上定义的羟基或羟基醚化或酯化; R5是C1-10烃脂族基团; 被芳基取代的C1-10烃脂族基，对上述R2定义的取代芳基或卤素; 或环烷基，取代的环烷基，芳基，取代的芳基或芳族杂环，全部如上述R2所定义; 或其生理上可接受的盐，当R1为OH时，具有有价值的药理学性质。