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1.发明授权Novel prostaglandin intermediates and process for the production thereof 失效新的PROSTAGLANDIN中间件及其生产工艺
公开(公告)号：US3998852A
公开(公告)日：1976-12-21
申请号：US541188
申请日：1975-01-15
IPC分类号： C07C405/00 , C07D309/22
CPC分类号： C07C405/00
摘要： Novel prostaglandin intermediates and process for the production thereof. Compounds, and process for the production thereof, useful in the production of (dl)-[1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4.alpha.-tetrahydropyranyloxycyclopent-1.alpha.-yl] acetaldehyde hemiacetal and [1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4.alpha.-tetrahydropyranyloxycyclopent-1.alpha.-yl] acetaldehyde hemiacetal.
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2.发明授权Processes and intermediates for making 16-phenoxy- and 16-substituted phenoxy-prostatrienoic acid derivatives and their stereoisomers 失效制备16-苯氧基和16-取代的苯氧基 - 前列腺烯酸衍生物及其立体异构体的方法和中间体
公开(公告)号：US4912235A
公开(公告)日：1990-03-27
申请号：US203398
申请日：1988-06-07
IPC分类号： C07C405/00 , C07F7/18 , C07D315/00 , C07C177/00
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0025 , C07C405/0033 , C07C405/0041 , C07F7/1856
摘要： This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.
摘要翻译： 本发明涉及以其立体异构体或其混合物的形式制备式I化合物（I）的方法，其中R是氢，低级烷基; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，波浪线代表α或β构型，条件是当一个波浪线是α时，另一个是β，或药学上可接受的无毒的盐 其中R是氢的化合物; 用于制备这些化合物的新型中间体; 制造中间体的方法; 和其中R是甲基且X是氢的式I化合物的立体异构体及其制备方法。
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3.发明授权Processes and intermediates for making 16-phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives and their stereoisomers 失效制备16-苯氧基和16-取代的苯氧基 - 前列腺烯酸衍生物及其立体异构体的方法和中间体
公开(公告)号：US4780562A
公开(公告)日：1988-10-25
申请号：US776063
申请日：1985-09-13
IPC分类号： C07C405/00 , C07C17/00
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0033 , C07C405/0041
摘要： This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.
摘要翻译： 本发明涉及以其立体异构体或其混合物的形式制备式I化合物（I）的方法，其中R是氢，低级烷基; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，波浪线代表α或β构型，条件是当一个波浪线是α时，另一个是β，或药学上可接受的无毒的盐 其中R是氢的化合物; 用于制备这些化合物的新型中间体; 制造中间体的方法; 和其中R是甲基且X是氢的式I化合物的立体异构体及其制备方法。
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公开(公告)号：US4055564A
公开(公告)日：1977-10-25
申请号：US716727
申请日：1976-08-23
IPC分类号： C07C405/00 , C07D7/02 , C07C61/06
CPC分类号： C07C405/00
摘要： Novel prostaglandin intermediates and process for the production thereof. Compounds, and process for the production thereof, useful in the production of (dl)-[1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4.alpha.-tetrahydropyranyloxy-cyclopent-1.alpha.-yl] acetaldehyde hemiacetal and [1.alpha.-hydroxy-3.beta.-(3S-tetrahydropyranyloxy-trans-1-octenyl)-4.alpha.-tetrahydropyranyloxycyclopent-1.alpha.-yl] acetaldehyde hemiacetal.
摘要翻译： 新型前列腺素中间体及其制备方法。 化合物及其制备方法，可用于制备（dl） - [1α-羟基-3β-（3S-四氢吡喃氧基 - 反-1-辛烯基）-4α-四氢吡喃氧基 - 环戊-1-基] ]乙醛半缩醛和[1α-羟基-3β-（3S-四氢吡喃氧基 - 反-1-辛烯基）-4α-四氢吡喃氧基环戊-1α-基]乙醛半缩醛。
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5.发明授权(dl)-16-Phenoxy- and 16-substituted phenoxy-9-keto prostatrienoic acid derivatives and processes for the production thereof 失效（dl）-16-苯氧基 - 和16-取代的苯氧基-9-酮前列腺烯酸衍生物及其制备方法
公开(公告)号：US4178457A
公开(公告)日：1979-12-11
申请号：US922957
申请日：1978-07-10
IPC分类号： A61K31/23 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , Y02P20/582
摘要： Novel 16-phenoxy and 16-(o, m or p)-substituted phenoxy derivatives of (dl)-9-keto-11.alpha.,15.alpha.-dihydroxy-17,18,19,20-tetranorprosta-4,5,13-trans-trienoic acid, the pharmaceutically acceptable, non-toxic lower alkyl esters and salts thereof and processes for the production of such compounds. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals where prostaglandins are indicated. They are particularly useful as inhibitors of gastric acid secretion; and as agents for the control of asthmatic attack, because of their bronchodilating activity.
摘要翻译： （dl）-9-酮-11α，15α-二羟基-17,18,19,20-四前列腺素-4,5,13的新的16-苯氧基和16-（o，m或p） - 取代的苯氧基衍生物 - 反式三烯酸，其药学上可接受的，无毒的低级烷基酯及其盐及其制备方法。 这些化合物具有前列腺素样活性，因此可用于治疗表达前列腺素的哺乳动物。 它们特别可用作胃酸分泌抑制剂; 并且作为控制哮喘发作的药剂，因为它们的支气管扩张活性。
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6.发明授权Processes and intermediates for making 16-phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives 失效制备16-苯氧基和16-取代的苯氧基 - 前列腺烯酸衍生物的方法和中间体
公开(公告)号：US4804787A
公开(公告)日：1989-02-14
申请号：US785934
申请日：1985-10-09
IPC分类号： C07C405/00 , C07F7/18 , C07C41/00
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041 , C07F7/1856
摘要： This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.
摘要翻译： 本发明涉及制备下式化合物的对映异构体或外消旋混合物的方法，其中R是氢，其中R是氢的化合物的低级烷基或药学上可接受的无毒盐; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，波浪线表示α或β构型，条件是当一个波浪线是α时，另一个是β。 用于制备这些化合物的新型中间体; 和制备中间体的方法。
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7.发明授权9-oxo-15.alpha.-hydroxy-16-phenoxy and 16-substituted phenoxy 17,18,19,20-tetranorprosta-4,5,13,(E)-trienoates 失效9-氧代-15α-羟基-16-苯氧基和16-取代的苯氧基17,18,19,20-四前驱体-4,5,13，（E） - 三烯酸酯
公开(公告)号：US4618696A
公开(公告)日：1986-10-21
申请号：US636058
申请日：1984-07-31
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; and X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..
摘要翻译： 本发明涵盖下式的化合物，其中R是氢，其中R是氢的化合物的低级烷基或药学上可接受的无毒盐; X为氢，卤素，三氟甲基，低级烷基或低级烷氧基; 波浪线表示α或β配置，条件是当一条波浪线为α时，另一条波长为β。
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8.发明授权Processes and intermediates for making 16-phenoxy and 16-substituted phenoxy-prostatrienoic acid derivatives 失效制备16-苯氧基和16-取代的苯氧基 - 前列腺烯酸衍生物的方法和中间体
公开(公告)号：US4600785A
公开(公告)日：1986-07-15
申请号：US564386
申请日：1983-12-22
IPC分类号： C07B57/00 , A61K31/557 , A61K31/5575 , A61P1/04 , C07B31/00 , C07B55/00 , C07C5/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/36 , C07F7/08 , C07F7/18 , C07C177/00
CPC分类号： C07F7/1856 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041
摘要： This invention relates to a process for making an enantiomer or racemic mixture of a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is a .alpha. the other is .beta.; novel intermediates useful for preparing these compounds; and processes for making the intermediates.
摘要翻译： 本发明涉及制备下式化合物的对映异构体或外消旋混合物的方法，其中R是氢，其中R是氢的化合物的低级烷基或药学上可接受的无毒盐; X是氢，卤素，三氟甲基，低级烷基或低级烷氧基，波浪线表示α或β构型，条件是当一个波浪线是α时，另一个是β; 用于制备这些化合物的新型中间体; 和制备中间体的方法。
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公开(公告)号：US4234491A
公开(公告)日：1980-11-18
申请号：US022667
申请日：1979-03-22
申请人： Gary F. Cooper , Albert R. Van Horn
发明人： Gary F. Cooper , Albert R. Van Horn
IPC分类号： C07C51/56 , C07D317/26 , C07D317/12
CPC分类号： C07D317/26 , C07C51/56
摘要： The tricyclic intermediate ##STR1## is prepared in a three step sequence from the bicyclic intermediate ##STR2## The key step of this process involves the addition of a Grignard reagent to a mixed anhydride. Tricyclic compound of formula (I) may be readily converted by known methods to valuable steroids.
摘要翻译： 三环中间体（I）以三步法从双环中间体（II）制备。该方法的关键步骤包括向混合酸酐中加入格氏试剂。 式（I）的三环化合物可以通过已知方法容易地转化为有价值的类固醇。
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公开(公告)号：US4158012A
公开(公告)日：1979-06-12
申请号：US916443
申请日：1978-06-19
申请人： Gary F. Cooper , Albert R. Van Horn
发明人： Gary F. Cooper , Albert R. Van Horn
IPC分类号： C07C69/716 , A61K31/585 , C07C49/597 , C07C49/613 , C07C51/56 , C07C59/205 , C07D317/26 , C07J1/00 , C07J17/00 , C07C61/38
CPC分类号： C07D317/26 , C07C51/56
摘要： The tricyclic intermediate ##STR1## is prepared in a three step sequence from the bicyclic intermediate ##STR2## The key step of this process involves the addition of a Grignard reagent to a mixed anhydride. Tricyclic compound of formula (I) may be readily converted by known methods to valuable steroids.
摘要翻译： {PG，1三环中间体{r1 {tc，1 {tr，29 {rb {rd，dd00335588 {db，b {sd，11 {sb，15 O {A，5 {M，1 {A，2 {LS ，8 {SD，26 {SB，4 O {A，1 {BN，D {SD，5 {SB，15 O {A，2 {BL，8 {BL，B {RD，BFF1 {MR，1 {RD ，335588BBDD / 1 {A，2 {RD，00335588BB {A，4 {BN，0 {A，4 {RD，335588CCCC {A，2 {DB，0 {US，5 {SB， {PS {PS从三环中间体{r1 {tc，1 {tr，28 {rb {rd，033 {a，1 {sd，15 {sb，4 CO {HD 2 { A，3 {BU，00 {RD，DD00335588BB {A，2 {DB，B {SD，11 {SB，14 O {A，5 {BN，0 {A，5 {RD，335588CCCC {A，2 {DB ，0 {US，5 {SB，4 O {A，5 {BU，88 {SD，15 {SB，4 H {RE（II）{PS {PS）该过程的关键步骤涉及添加格氏试剂 与混合酸酐反应。 式（I）的三环化合物可以通过已知方法容易地转化为有价值的类固醇。
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