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    • 1. 发明专利
    • Optically active imidazolylpropanediol derivative and its preparation
    • 光学有效的咪唑并吡喃衍生物及其制备
    • JPS58203974A
    • 1983-11-28
    • JP5332783
    • 1983-03-28
    • Sumitomo Chem Co Ltd
    • SAJI KITAROUSATOU RENZOUAONO SHIYUNJIICHINOSE KATSUAKIOKUDA TAKAOATAMI TOSHIO
    • C07D233/60A61K31/415A61P31/04A61P31/10
    • NEW MATERIAL:(R)-2-(2,4-Dichlorophenyl)-1-(imidazol-1-yl)-2,3-propanediol of formula I .
      USE: A synthetic intermediate of optically active imidazolylalkylthiopropanol derivative having strong mycostatic activity.
      PROCESS: The optically active diol derivative of formula I can be prepared e.g. by (1) reacting the racemic imidazolyldiol derivative of formula II with an optically active carboxylic acid or its reactive derivative, preferably the optically active carboxylic acid of formula III to obtain the 1:1 mixture of two kinds of diastereomer esters, (2) separating the objective ester from the diastereomer mixture by chromatography, fractional recrystallization, etc., and (3) hydrolyzing the resultant ester.
      COPYRIGHT: (C)1983,JPO&Japio
    • 新材料:式I的(R)-2-(2,4-二氯苯基)-1-(咪唑-1-基)-2,3-丙二醇。 用途:具有很强的静电活性的光学活性咪唑基烷基硫代丙醇衍生物的合成中间体。 方法:式I的光学活性二醇衍生物可以例如制备。 通过(1)使式II的外消旋咪唑烷二醇衍生物与光学活性羧酸或其反应性衍生物,优选式III的光学活性羧酸反应,得到两种非对映体酯的1:1混合物,(2)分离 通过色谱法,分级重结晶等来自非对映异构体混合物的目标酯,和(3)水解所得酯。
    • 2. 发明专利
    • Optically active imidazolylmethyloxirane derivative and its preparation
    • 光学活性的咪唑啉衍生物衍生物及其制备
    • JPS58203988A
    • 1983-11-28
    • JP5332683
    • 1983-03-28
    • Sumitomo Chem Co Ltd
    • SAJI KITAROUSATOU RENZOUAONO SHIYUNJIICHINOSE KATSUAKIOKUDA TAKAOATAMI TOSHIO
    • C07C57/58C07B31/00C07B57/00C07C51/00C07C67/00C07D405/06
    • NEW MATERIAL:(R)-2-(2,4-Dichlorophenyl)-2-(imidazol-1-yl)methyloxirane of formula I .
      USE: A synthetic intermediate of optically active imidazolylalkylthiopropanol derivative having strong antifungal activity.
      PROCESS: The racemic isomer of the imidazolyldiol derivative of formula II is made to react with an optically active carboxylic acid (or its reactive derivative) (preferably the compound of formula III) to obtain two kinds of diastereomer esters, from which the objective ester is separated. The separated ester is hydrolyzed under alkaline condition, and the resultant optically active imidazolyldiol derivative of formula IV is methylated with methanesulfonyl chloride, and without isolating from the reaction system, treated with an alkali to obtain the objective compound of formula I .
      COPYRIGHT: (C)1983,JPO&Japio
    • 新材料:式I的(R)-2-(2,4-二氯苯基)-2-(咪唑-1-基)甲基环氧乙烷。 用途:具有强抗真菌活性的光学活性咪唑基烷基硫代丙醇衍生物的合成中间体。 方法:使式II的咪唑烷二醇衍生物的外消旋异构体与光学活性羧酸(或其反应性衍生物)(优选式III化合物)反应,得到两种非对映异构体酯,其中目标酯为 分开 将分离的酯在碱性条件下水解,将得到的式Ⅳ的旋光性咪唑烷二醇衍生物用甲磺酰氯甲基化,不用从反应体系中分离,用​​碱处理,得到目的化合物Ⅰ。
    • 5. 发明专利
    • Antiulcer agent
    • 抗体药剂
    • JPS5748912A
    • 1982-03-20
    • JP12497580
    • 1980-09-08
    • Sumitomo Chem Co Ltd
    • SUGIE AKIHIKOKAWAKAMI HAJIMEFUKUDA TOKUOONO KEIICHIAONO SHIYUNJIKATSUBE SUMIMOTO
    • A61K31/19A61K31/215A61P1/04
    • NEW MATERIAL:A compound of formula I (R
      1 is H or 1W4C lower alkyl) and a salt thereof.
      EXAMPLE: The compound of formula II.
      USE: A chemically stable antiulcer agent, having excellent selectivity, with little side effects, and useful for diseases, e.g. duodenal ulcer, and administrable orally and parenterally.
      PROCESS: As shown in the reaction formulas, a cyclohexene derivative of formula III is subjected to the oxidative ring cleavage to give a dialdehyde derivative of formula IV, which is then subjected to the intramolecular aldol reaction to afford a compound of formula V. The resultant compound of formula V is then reacted with a wittig reagent to give a compound of formula VI, which is subsequently reduced to afford a compound of formula VII. The protecting group of the ketal ketonic group expressed by W is then removed from the resultant compound of formula VII to give a compound of formula VIII, which is then reacted with a Wittig reagent to afford the compound of formula I.
      COPYRIGHT: (C)1982,JPO&Japio
    • 新材料:式Ⅰ化合物(R1为H或1-4C低级烷基)及其盐。 实施例:式II化合物。 用途:化学稳定的抗溃疡剂,具有优异的选择性,副作用小,可用于疾病,例如 十二指肠溃疡,口服和肠胃外给药。 方法:如反应式所示,将式III的环己烯衍生物进行氧化环切割,得到式IV的二醛衍生物,然后将其进行分子内醛醇缩合反应,得到式V化合物。所得物 然后将式V化合物与无机试剂反应,得到式Ⅵ化合物,随后将其还原,得到式Ⅶ化合物。 然后将由W表示的缩酮酮基团的保护基从所得到的式VII化合物中除去,得到式VIII化合物,然后与Wittig试剂反应,得到式I化合物。