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    • 2. 发明授权
    • Method for preparing prostaglandins
    • 前列腺素的制备方法
    • US4088536A
    • 1978-05-09
    • US772019
    • 1977-02-25
    • Charles J. Sih
    • Charles J. Sih
    • C07C405/00C07D303/32C07D309/12C07F1/02C07F1/08C07F5/06C12D1/02
    • C07F1/02C07C405/00C07D303/32C07D309/12C07F1/08C07F5/066Y10S435/913Y10S435/933
    • Racemic 15-deoxo, 11,15-deoxy and other prostaglandins and methods for preparing the same. The initial reactant is lithium cyclopentadiene which is reacted with ethyl-7-bromoheptanoate to give the alkylated diene which in turn is oxygenated to a mixture of hydroxycyclopentenones. 2-(6'-carboethoxyhexyl)-4-hydroxy-cyclopenten-1-one is chromatographically recovered from the mixture and reacted with dihydropyran to give the tetrahydropyranyl ether which is then reacted with 1-lithium-1-trans-octene in the presence of tri-n-butylphosphine-copper iodide to produce racemic 15-deoxy-prostaglandin E.sub.1 ethyl ester which is chromatographically recovered. The ester is converted to the corresponding prostaglandin by the action of an esterase-producing microorganism.
    • 外消旋15-脱氧,11,15-脱氧等前列腺素及其制备方法。 初始反应物是环戊二烯锂,其与7-溴庚酸乙酯反应,得到烷基化二烯,其又被氧化成羟基环戊烯酮的混合物。 将2-(6'-羰乙氧基己基)-4-羟基 - 环戊烯-1-酮从混合物中色谱回收并与二氢吡喃反应,得到四氢吡喃基醚,然后在存在下与1-锂-1-反式 - 辛烯反应 的三正丁基膦 - 碘化铜,制备色谱回收的外消旋15-脱氧 - 前列腺素E1乙酯。 通过产酯酶微生物的作用将酯转变成相应的前列腺素。
    • 10. 发明授权
    • Physiologically active novel substance mutastein and process for its
production
    • 生理活性的新型物质mutastin及其生产工艺
    • US4436725A
    • 1984-03-13
    • US352069
    • 1982-02-24
    • Akira Endo
    • Akira Endo
    • A61K36/06A61P1/02C07G99/00C12P1/02C12R1/66A61K35/00A61K7/16C12D1/02
    • C12R1/66C12P1/02
    • A physiologically active novel substance designated as Mutastein is disclosed, which has the following specific physiological properties:(1) it has a molecular weight of at least 200,000, and when subjected to gel-filtration with Sephadex G-100 and Sephallose 6B, it will be eluted in the void volume;(2) its ultraviolet spectrum: FIG. 1;(3) its infrared spectrum: FIG. 2;(4) it has a proteinous nature and contains about 10% of saccharide;(5) it is soluble in water and a saline solution, but it will be salted out from a saturated solution containing about 30% of ammonium salfate; and it is insoluble in acetone, ethanol, ethylacetate and benzene,(6) it dissolves in a buffer solution having a pH 7 or over, but it precipitates at a pH of from 3 to 3.5,(7) it is stable when heat-treated at pH 9, at 100.degree. C. for 10 minutes,(8) its elementary analysis: C: about 44%, H: about 7%, and N: about 12%,(9) its color reactions: Phenol-surfuric acid color reaction (orange), and Folin's color reaction (blue). This substance can be prepared by culturing the Mutastein-producing strain belonging to the genus Aspergillus, and isolating the Mutastein from the culture medium.
    • 公开了一种命名为Mutastein的生理活性新物质,其具有以下具体的生理特性:(1)其分子量至少为20万,当用Sephadex G-100和Sephallose 6B进行凝胶过滤时,将会是 在空隙体积中洗脱; (2)其紫外光谱: 1; (3)其红外光谱: 2; (4)具有蛋白质性质,含有约10%的糖类; (5)它可溶于水和盐水溶液,但会从含有约30%硫酸铵的饱和溶液中脱盐; 它不溶于丙酮,乙醇,乙酸乙酯和苯,(6)溶于pH7或以上的缓冲溶液中,但在3〜3.5的pH下析出,(7) 在pH 9,100℃下处理10分钟,(8)其元素分析:C:约44%,H:约7%,N:约12%,(9)其显色反应:苯酚 - 酸性反应(橙色)和Folin的颜色反应(蓝色)。 该物质可以通过培养属于曲霉属的产生Mutaminin的菌株并从培养基中分离出Mutastein来制备。