METHODS OF ASSAYING TROPOLONE
    2.
    发明申请

    公开(公告)号:WO2019113050A1

    公开(公告)日:2019-06-13

    申请号:PCT/US2018/063822

    申请日:2018-12-04

    CPC classification number: G01N33/64 C07C45/79 C07C49/717

    Abstract: Disclosed herein are methods useful for detecting and/or quantifying tropolone in samples, e.g., generated during the production of and in final formulations of a product, e.g., a recombinant protein, e.g., an antibody. Tropolone and derivatives thereof (cycloheptatriene ketones) are separated from a mixture by adding a partially or fully fluorinated alkyl or aryl (e.g. pentafluorophenylpropyl), which (covalently) binds the tropolone-like compound. Then it is assayed via UV or tandem mass spectrometry. A reaction mixture of tropolone-like compounds and fluorinated alkyl or aryl is also disclosed.

    TROPOLONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS
    4.
    发明申请
    TROPOLONE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 审中-公开
    TROPOLONE衍生物和药物组合物

    公开(公告)号:WO01089504A1

    公开(公告)日:2001-11-29

    申请号:PCT/JP2001/004362

    申请日:2001-05-24

    Abstract: Excellent 12-lipoxygenase inhibitors containing as the active ingredient tropolone derivatives of the general formula (1) or salts thereof. In said formula wherein R is hydrogen or optionally substituted C3-10 alkenyl; R is hydrogen, C1-6 alkyl, optionally substituted C3-10 alkenyl, or alkynyl; R is hydrogen; R is hydrogen or C1-6 alkyl; and R is hydrogen or a group of the general formula (2): -(CH2)nNR R (wherein n is an integer of 1 to 6; and R and R are each independently hydrogen, alkyl, or aralkyl, or alternatively R and R together with the nitrogen atom adjacent thereto may represent optionally substituted 5- or 6-membered cyclic amino), with the proviso that the compound wherein R , R , R , R and R are simultaneously hydrogen is excepted.

    Abstract translation: 含有作为活性成分的通式(1)的托普洛尔衍生物或其盐的优异的12-脂氧合酶抑制剂。 在所述式中,其中R 1是氢或任选取代的C 3-10烯基; R 2是氢,C 1-6烷基,任选取代的C 3-10烯基或炔基; R 3是氢; R 4是氢或C 1-6烷基; 和R 5为氢或通式(2)的基团: - (CH 2)n NR 6 R 7(其中n为1至6的整数; R 6和R 7为 各自独立地为氢,烷基或芳烷基,或者R 6和R 7与其相邻的氮原子一起可以表示任选取代的5-或6-元环状氨基),条件是其中 R 1,R 2,R 3,R 4和R 5同时为氢。

    PROCESS FOR PRODUCING HINOKITIOL
    10.
    发明申请
    PROCESS FOR PRODUCING HINOKITIOL 审中-公开
    生产工艺的过程

    公开(公告)号:WO99050215A1

    公开(公告)日:1999-10-07

    申请号:PCT/JP1999/001583

    申请日:1999-03-29

    Abstract: A process for producing hinokitiol which comprises obtaining 1-isopropylcyclopentadiene from cyclopentadiene and an isopropylating agent represented by the general formula R-X (wherein R represents isopropyl; and X represents halogeno, etc.) (the step 1); reacting the obtained product with a dihaloketene to give a ketene-adduct (the step 2); and then decomposing this ketene-adduct (the step 3); wherein the above step 1 involves the following three steps: (a) the step of preparing a cyclopentadienyl metal; (b) the step of isopropylating the cyclopentadienyl metal in an aprotic polar solvent to give isopropylcyclopentadiene; and (c) the step of isomerizing 5-isopropylcyclopentadiene contained in the product selectively into 1-isopropylcyclopentadiene under heating.

    Abstract translation: 制备桧醇的方法,其包括从环戊二烯获得1-异丙基环戊二烯和由通式R-X表示的异丙基化剂(其中R表示异丙基; X表示卤代等)(步骤1); 使所得产物与二卤代烯酮反应,得到乙烯酮加合物(步骤2); 然后分解该乙烯酮加合物(步骤3); 其中上述步骤1涉及以下三个步骤:(a)制备环戊二烯基金属的步骤; (b)在非质子传递极性溶剂中异丙基化环戊二烯基金属以得到异丙基环戊二烯的步骤; 和(c)在加热下将产物中所含的5-异丙基环戊二烯选择性异构化成1-异丙基环戊二烯的步骤。

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