11-Deoxy 15-methyl prostaglandin E.sub.1
    3.
    发明授权
    11-Deoxy 15-methyl prostaglandin E.sub.1 失效
    11-脱氧15-甲基前列腺素E {HD 1

    公开(公告)号:US3972917A

    公开(公告)日:1976-08-03

    申请号:US473604

    申请日:1974-05-28

    申请人: Donald P. Strike

    发明人: Donald P. Strike

    CPC分类号: C07C405/00 Y10S514/826

    摘要: 11-Deoxy-prostaglandin compounds having a lower alkyl group at position-15 are prepared from PGA.sub.2 esters and 15-epimers. These 15-lower alkyl-11-deoxy prostaglandins possess bronchodilative ability.

    摘要翻译: 在15位具有低级烷基的11-脱氧 - 前列腺素化合物由PGA2酯和15-差向异构体制备。 这些15-低级烷基-11-脱氧前列腺素具有支气管扩张能力。

    Dl-strigol intermediate
    4.
    发明授权
    Dl-strigol intermediate 失效
    Dl-strigol中间体

    公开(公告)号:US3972916A

    公开(公告)日:1976-08-03

    申请号:US532759

    申请日:1974-12-13

    申请人: Charles J. Sih

    发明人: Charles J. Sih

    IPC分类号: C07D307/93 C07C61/38

    CPC分类号: C07D307/93

    摘要: A process for preparing dl-strigol, a potent seed germination agent, which comprises preparing the 2-bromomethyl-substituted methyl ester of 2,6,6-trimethylcyclohex-1-en-3-one-1-carboxylic acid, alkylating and cyclizing the said compound with an excess of dimethyl sodiomalonate to obtain methyl 1,4-diketo-7,7-dimethyl-4,5,6,7-tetrahydroindane-2-carboxylate and its enol, subjecting the said keto and enol forms of the compound, in admixture, to alkylation with methyl bromoacetate followed by acidic hydrolysis and spontaneous decarboxylation to obtain methyl 1,4-diketo-7,7-dimethyl-4,5,6,7-tetrahydroindane-2-acetic acid, reducing the said acetic with a hydride reducing agent and recovering and separating the resulting 1,4-cis and trans-dihydroxy-7,7-dimethyl-4,5,6,7-tetrahydroindane-2-acetic acid lactones, formylating each of the cis and trans .gamma. lactones, alkylating the respective resulting hydroxy methylene lactones with bromobutenolide and recovering dl-strigol, dl-4'-epi-strigol, dl-4-epi-strigol and dl-4,4'-diepi-strigol.New compounds useful as intermediates in the above process are also shown.

    摘要翻译: 一种制备有效种子萌发剂的dl-strigol的方法,其包括制备2,6,6-三甲基环己-1-烯-3-酮-1-羧酸的2-溴甲基取代的甲酯,烷基化和环化 所述化合物与过量的二甲基磺酸钠反应得到1,4-二酮-7,7-二甲基-4,5,6,7-四氢茚满-2-甲酸甲酯及其烯醇,使所述酮和烯醇形式的 化合物,混合物与溴乙酸甲酯烷基化,然后酸性水解和自发脱羧,得到1,4-二酮-7,7-二甲基-4,5,6,7-四氢茚满-2-乙酸甲酯,将所述 乙酸与氢化物还原剂反应并回收并分离得到的1,4-顺式和反式二羟基-7,7-二甲基-4,5,6,7-四氢茚满-2-乙酸内酯,将每个顺式和 反式γ-内酯,用溴丁烯内酯对相应的所得羟基亚甲基内酯进行烷基化,并回收dl-strigol,dl-4'-表柔比星,d l-4-表柔比星和dl-4,4'-二苯甲醚。

    13,14-Dihydro-16-fluoro prostaglandin E.sub.1 analogs
    5.
    发明授权
    13,14-Dihydro-16-fluoro prostaglandin E.sub.1 analogs 失效
    13,14-二氢-16-氟前列腺素E {HD 1 {B类似物

    公开(公告)号:US3969376A

    公开(公告)日:1976-07-13

    申请号:US551692

    申请日:1975-02-21

    CPC分类号: C07D307/935 C07C405/00

    摘要: Prostaglandin-type compounds with one or two fluoro substituents at the C-16 position are disclosed, with processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.

    摘要翻译: 公开了在C-16位具有一个或两个氟取代基的前列腺素型化合物及其制备方法。 这些化合物可用于各种药理学目的,包括抗溃疡,抑制血小板聚集,增加鼻通气,术中劳动诱导和伤口愈合。

    1-Carboxymethyl-3-chloroadamantane
    6.
    发明授权
    1-Carboxymethyl-3-chloroadamantane 失效
    1-羧甲基-3-氯金刚烷

    公开(公告)号:US3966800A

    公开(公告)日:1976-06-29

    申请号:US528399

    申请日:1974-11-29

    IPC分类号: C07C53/23 C07C61/38

    CPC分类号: C07C53/23

    摘要: The compound, 1-carboxymethyl-3-chloroadamantane, is useful as a plant growth stimulator and as an intermediate for preparing other useful compounds. The compound, 1-carboxymethyl-3-chloroadamantane, is prepared by reacting 1-aoamantylacetic acid with a hydrogen halide or a metal halide, in 70-98 wt. % sulfuric acid, in carbon tetrachloride or cyclohexane, and in the presence of t-butanol.

    摘要翻译: 化合物1-羧甲基-3-氯金刚烷可用作植物生长刺激剂和作为制备其它有用化合物的中间体。 1-羧甲基-3-氯金刚烷的化合物是通过使1-金刚烷基乙酸与卤化氢或金属卤化物反应制得的,其为70-98wt。 %硫酸,在四氯化碳或环己烷中,并在叔丁醇存在下进行。

    Prostaglandin intermediate
    8.
    发明授权
    Prostaglandin intermediate 失效
    前列腺素中间体

    公开(公告)号:US3959263A

    公开(公告)日:1976-05-25

    申请号:US480788

    申请日:1974-06-19

    摘要: Prostaglandin derivatives of the formula ##SPC1##In which R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each are hydrogen or lower alkyl, X is hydroxy and Y is hydrogen or X and Y together are oxo, Z is CH.sub.2 CH.sub.2 or trans CH=CH, m is an integer from one to three and n is an integer from two to five, with the proviso that at least one of R.sup.4, R.sup.5 or R.sup.6 is hydrogen, are disclosed together with a process for their preparation. The compounds in which Z is CH.sub.2 CH.sub.2 and the process are new. The new derivatives possess hypotensive, antihypertensive, bronchospasmolytic, gastric acid secretion inhibiting, abortifacient, estrus synchronizing and ovulation regulating properties. These compounds also inhibit the aggregation of platelets and promote the disaggregation of aggregated platelets. Methods for their use are also disclosed.

    摘要翻译: 式IV的前列腺素衍生物R4,R5,R6和R7各自为氢或低级烷基,X为羟基,Y为氢或X和Y一起为氧代,Z为CH 2 CH 2或反式CH = CH,m为 一至三个,n为二至五的整数,条件是R4,R5或R6中的至少一个为氢,并与其制备方法一起公开。 其中Z为CH 2 CH 2并且该方法是新的化合物。 新衍生物具有降压,降压,支气管痉挛,胃酸分泌抑制,堕胎,发情同步和排卵调节特性。 这些化合物还抑制血小板的聚集并促进聚集的血小板的解聚。 还公开了它们的使用方法。

    4,5-Cis-didehydro-PGF.sub.1.sub..alpha.  analogs
    10.
    发明授权
    4,5-Cis-didehydro-PGF.sub.1.sub..alpha. analogs 失效
    4,5-Cis-didehydro-PGF {HD 1 {301 {B {0 analogs

    公开(公告)号:US3933889A

    公开(公告)日:1976-01-20

    申请号:US440629

    申请日:1974-02-07

    摘要: This invention is a group of 4,5-didehydro PG.sub.1 (prostaglandin-type) analogs having variable chain length, branching and fluoro substitution in the hydroxy-substituted side-chain, and processes for making them. These compounds are useful for a variety of pharmacological purposes, including anti-ulcer, inhibition of platelet aggregation, increase of nasal patency, labor inducement at term, and wound healing.

    摘要翻译: 本发明是一组在羟基取代的侧链具有可变链长,支链和氟取代的4,5-二脱氧PG1(前列腺素型)类似物及其制备方法。 这些化合物可用于各种药理学目的,包括抗溃疡,抑制血小板聚集,增加鼻通气,术中劳动诱导和伤口愈合。