PROCESS FOR PREPARING EXTRA PURE 2, 6-DIISOPROPYL PHENOL
    3.
    发明公开
    PROCESS FOR PREPARING EXTRA PURE 2, 6-DIISOPROPYL PHENOL 有权
    用于生产超纯2,6-二异丙基

    公开(公告)号:EP2516369A4

    公开(公告)日:2013-05-29

    申请号:EP10853576

    申请日:2010-08-10

    IPC分类号: C07C39/06 A61K31/05 A61P23/00

    摘要: Disclosed herein is a process for the preparation of highly pure 2,6-diisopropyl phenol (Formula I), which comprises reacting p-hydroxy benzoic acid (Formula II) with an alkylating agent in presence of aq. mineral acid followed by basification and subsequent washings to yield 4-hydroxy-3,5-diisopropylbenzoic acid (Formula III) free of dimer impurity, 4,4'-oxydibenzoic acid of Formula IV, ether impurity 3,5-di(propan-2-yl)-4-(propan-2-yloxy)benzoic acid of Formula V and the monoalkylated impurity 4-hydroxy-3-(propan-2-yl)benzoic acid of Formula VI; and decarboxylating 4-hydroxy-3,5-diisopropylbenzoic acid (Formula III) in presence of high boiling solvent and sodium hydroxide as a catalyst at high temperature to yield 2,6-diisopropyl phenol substantially free of ether impurity 1,3-di(propan-2-yl)-2-(propan-2-yloxy)benzene of Formula VII and monoalkylated phenol impurity 2-(propan-2-yl) phenol of Formula VIII. Propofol prepared by the process of the present invention is suitable for pharmaceutical use.

    PROCESS FOR PRODUCING TRIPHENYLENE COMPOUND AND CRYSTAL OBTAINED BY THE PROCESS
    5.
    发明公开
    PROCESS FOR PRODUCING TRIPHENYLENE COMPOUND AND CRYSTAL OBTAINED BY THE PROCESS 审中-公开
    Verfahren zur Herstellung von Hexahydroxytriphenylen-Derivaten

    公开(公告)号:EP2177495A1

    公开(公告)日:2010-04-21

    申请号:EP08792270.4

    申请日:2008-08-06

    摘要: An object of the present invention is to provide a process for producing high-purity hydroxytriphenylenes in which not only inexpensive raw materials can be used but also no complicated steps of deprotection such as dealkylation, and reduction and the like are necessary, and which is thereby advantageous in industrial production. Also there is provided a novel crystal of 2,3,6,7,10,11-hexahydroxytriphenylene monohydrate, which has satisfactory thermal stability. The process for producing a compound represented by the general formula (2) is characterized by reacting a compound represented by the general formula (1) in the presence of a metal oxide comprising a metal selected from trivalent iron, pentavalent vanadium and hexavalent molybdenum and of a nonvolatile strong acid:

    wherein, Rs are each independently a hydrogen atom, a halogen atom, an alkyl group having 1 to 3 carbon atoms or an alkoxy group having 1 to 3 carbon atoms.

    摘要翻译: 本发明的目的是提供一种制备高纯度羟基三苯基的方法,其中不仅可以使用廉价的原料,而且不需要复杂的脱保护步骤如脱烷基化和还原等,从而 有利于工业生产。 还提供了具有令人满意的热稳定性的2,3,6,7,10,11-六羟基三亚苯一水合物的新晶体。 由通式(2)表示的化合物的制备方法的特征在于使通式(1)表示的化合物在包含选自三价铁,五价钒和六价钼的金属的金属氧化物存在下反应, 非挥发性强酸:其中,R 5各自独立地为氢原子,卤素原子,碳原子数为1〜3的烷基或碳原子数为1〜3的烷氧基。

    PROCESS FOR PREPARATION OF 3,5-BISALKYLPHENOLS
    8.
    发明公开
    PROCESS FOR PREPARATION OF 3,5-BISALKYLPHENOLS 有权
    VERFAHREN ZUR HERSTELLUNG VON 3,5-BISALKYLPHENOLEN

    公开(公告)号:EP1319646A4

    公开(公告)日:2005-11-30

    申请号:EP01970181

    申请日:2001-09-21

    申请人: KOWA CO

    摘要: A process for preparing 3,5-bisalkylphenols (2) from carbinol compounds (1); carbinol compounds (1); and a process for preparation of the compounds (1): (1) (2) [wherein R is hydrogen, alkali metal, alkaline earth metal, or a hydroxyl-protecting group(except methyl); R is C1-5 lower alkyl or optionally substituted phenyl; and R and R are each independently lower alkyl, aralkyl, or aryl]. This invention enables efficient and safe preparation of various 3,5-bisalkylphenols including 3,5-diisopropylphenol (which is important as an intermediate in the synthesis of drugs and agricultural chemicals) in shorter steps at high purity in high yield, thus contributing to stable supply of the drugs and agricultural chemicals.

    摘要翻译: 从甲醇化合物(1)制备3,5-双烷基酚(2)的方法; 甲醇化合物(1); (1)的制备方法:(1)(2)[其中R 1为氢,碱金属,碱土金属或羟基保护基(除甲基以外); R 2是C 1-5低级烷基或任选取代的苯基; 并且R 3和R 4各自独立地为低级烷基,芳烷基或芳基]。 本发明能够以高收率以高纯度以较短步骤高效且安全地制备各种3,5-二烷基酚,包括3,5-二异丙基苯酚(其作为药物和农用化学品合成中的重要中间体),因此有助于稳定 药品和农药的供应。