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23 条记录 (耗时 0.028 秒)

    8-Aza-9-dioxothiaprostanoic acids
    1.
    发明授权
    8-Aza-9-dioxothiaprostanoic acids 失效
    8-氮杂-9-二氧代硫代雄磷酸

    公开(公告)号：US4087435A

    公开(公告)日：1978-05-02

    申请号：US769477

    申请日：1977-02-17

    申请人： Edward J. Cragoe, Jr. ,  James H. Jones ,  John B. Bicking

    发明人： Edward J. Cragoe, Jr. ,  James H. Jones ,  John B. Bicking

    IPC分类号： C07D275/02

    CPC分类号： C07D275/02 ,  C07C327/00 ,  Y10S514/822 ,  Y10S514/929

    摘要： Novel 8-aza-9-dioxothiaprostanoic acid compounds, their salts, and derivatives, are prepared from ethyl 7-(3-hydroxymethyl-2-isothiazolidinyl)-5-heptynoate S,S-dioxide by first hydrogenating the triple bond over a Lindlar catalyst, followed by mild oxidation, to produce the corresponding 3-formyl compound, which is condensed with the ylide prepared from dimethyl-(2-oxoheptyl)phosphonate to produce the .alpha.,.beta.-unsaturated ketone, followed by reduction to the corresponding carbinol, and ester hydrolysis. The compounds are useful especially for the treatment of patients with poorly functioning kidneys, as hypotensives, or as platelet aggregation inhibitors.

    摘要翻译： 通过首先在Lindlar上氢化三重键，从7-（3-羟甲基-2-异噻唑烷基）-5-庚炔酸S，S-二氧化物乙酸酯制备新的8-氮杂-9-二氧代硫代雄甾烷酸化合物，其盐和衍生物 催化剂，然后轻度氧化，产生相应的3-甲酰基化合物，其与由二甲基 - （2-氧代庚基）膦酸酯制备的内鎓盐缩合以产生α，β-不饱和酮，随后还原成相应的甲醇， 和酯水解。 该化合物特别适用于治疗肾功能不全的患者，作为低血糖剂或血小板聚集抑制剂。

    Interphenylene 11,12-secoprostaglandins
    5.
    发明授权
    Interphenylene 11,12-secoprostaglandins 失效
    亚苯基11,12-前列腺素

    公开(公告)号：US4175203A

    公开(公告)日：1979-11-20

    申请号：US968890

    申请日：1978-12-13

    申请人： Edward J. Cragoe, Jr. ,  John B. Bicking

    发明人： Edward J. Cragoe, Jr. ,  John B. Bicking

    IPC分类号： C07C65/40 ,  C07C243/38 ,  C07D309/12 ,  C07C177/00

    CPC分类号： C07C403/20 ,  C07C243/38 ,  C07C65/40 ,  C07D309/12 ,  C07C2101/14

    摘要： Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as a pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.

    摘要翻译： 通过乙酸乙酯或乙酸乙酯的叔丁酯的逐步烷基化制备11,12-前列腺素的新型间苯二酚衍生物。 一种这样的方法包括用强碱处理乙酰乙酸的叔丁酯以形成阴离子，然后用对 - （3-溴丙基）苯甲酸乙酯处理，得到4-（4-叔丁氧基羰基-5-氧代 - 己基）苯甲酸酯，随后将由此形成的苯甲酸酯的阴离子与1-氯-4-乙酰氧基壬烷反应，生成4-（4-乙酰基-4-叔丁氧基羰基-8-乙酰氧基十三烷基）苯甲酸乙酯，然后脱羧和碱水解 以产生所需产物4-（4-乙酰基-8-羟基十三烷基）苯甲酸，其可用作治疗肾衰竭患者和预防移植排斥的药物。