METHD OF PRODUCING 3,5-BISALKYLPHENOL

    公开(公告)号:JP2002167343A

    公开(公告)日:2002-06-11

    申请号:JP2001054802

    申请日:2001-02-28

    Applicant: KOWA CO

    Abstract: PROBLEM TO BE SOLVED: To obtain, efficiently and safely in a short process, and further with high purity and in high yield, 3,5-diisopropylphenol or the like which are important as a synthetic intermediate for medicines and agrochemicals. SOLUTION: 3,5-bisalkylphenol (2) and a carbinol compound (1) are obtained by the following reaction formula. [wherein, R1 represents H, an alkali metal atom, an alkali earth metal atom or a hydroxyl protecting group (except a methyl group); R2 may represent a 1-5C lower alkyl group or a phenyl group which may have a substitute; R3 and R4 may represent the same or different lower alkyl, aralkyl or aryl groups].

    Novel substituted pyrimidine derivative and medicine comprising the same
    4.
    发明专利
    Novel substituted pyrimidine derivative and medicine comprising the same 审中-公开
    新型取代的吡哩啶衍生物及其药物

    公开(公告)号:JP2011136942A

    公开(公告)日:2011-07-14

    申请号:JP2009297783

    申请日:2009-12-28

    Abstract: PROBLEM TO BE SOLVED: To provide a novel compound that exhibits an effect for promoting insulin secretion from a pancreas β cell and is useful as a preventive and/or therapeutic agent for diseases caused by hyperglycemia, for example, diabetes. SOLUTION: The novel compound is a substituted pyrimidine derivative represented by general formula (1) [wherein the ring A is an optionally substituted 5 to 10-membered heteroaryl group; Q is an oxygen atom or the like; R 1 is a methyl group or the like; R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are each independently a hydrogen atom or the like; m is an integer of 0-2; and n is an integer of 1-3] or a salt thereof, or a solvate thereof. COPYRIGHT: (C)2011,JPO&INPIT

    Abstract translation: 待解决的问题:提供一种具有促进胰腺β细胞胰岛素分泌的作用的新型化合物,可用作高血糖引起的疾病例如糖尿病的预防和/或治疗剂。 解决方案:新化合物是由通式(1)表示的取代嘧啶衍生物[其中环A是任选取代的5至10元杂芳基; Q是氧原子等; R 1是甲基等; R 2 ,R 3 ,R 4 ,R 5 ,R R 7,R SP< SP>,< SP> 9< SP>和R< SP> 10< SP>各自独立地为氢原子等; m是0-2的整数; n为1-3的整数)或其盐或其溶剂合物。 版权所有(C)2011,JPO&INPIT

    Optically active dibenzylamine derivative and method for producing the same
    6.
    发明专利
    Optically active dibenzylamine derivative and method for producing the same 有权
    光活性二苯胺衍生物及其制备方法

    公开(公告)号:JP2013136572A

    公开(公告)日:2013-07-11

    申请号:JP2012263933

    申请日:2012-12-03

    Abstract: PROBLEM TO BE SOLVED: To provide a low-molecular compound which has such an action as to decrease the amount of PCSK9 protein and increase the amount of LDL receptor, and to provide a medicine including the low-molecular compound as an active ingredient.SOLUTION: The medicine includes (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetate which is substantially optically-pure or a salt thereof, or solvates of them as an active ingredient.

    Abstract translation: 要解决的问题:提供具有降低PCSK9蛋白质量和增加LDL受体量的作用的低分子化合物,并提供包含低分子化合物作为活性成分的药物。 :该药物包括(S) - 反 - {4 - [({2 - [({1- [3,5-双(三氟甲基)苯基]乙基} {5- [2-(甲基磺酰基)乙氧基] - 基}氨基)甲基] -4-(三氟甲基)苯基}(乙基)氨基)甲基]环己基}乙酸乙酯,其基本上为光学纯的或其盐,或它们的溶剂合物作为活性成分。

    PRODUCTION OF 3-(2',4'-DISUBSTITUTED PHENYL) PYRIDINE

    公开(公告)号:JPH03232857A

    公开(公告)日:1991-10-16

    申请号:JP2611390

    申请日:1990-02-07

    Applicant: KOWA CO

    Abstract: PURPOSE:To obtain the subject compound in high yield in a short process and under a modest condition by using diethyl-(3-pyridyl)borane and 2,4-disubstituted bromobenzene as starting raw materials, a specific solvent and a specific base and subjecting to a heating reaction in the presence of Pd catalyst. CONSTITUTION:Readily available diethyl-(3-pyridyl)borane and 2,4-disubstituted bromobenzene expressed by formula I [R is nitro or NHCOR (R is lower alkyl or N-protected amino lower alkyl); R is lower alkoxy] are reacted together with potassium carbonate and a base of tetraalkylammonium halide in dimethylformamide solvent in an inert gas atmosphere such as N2 gas in the presence of Pd catalyst preferably under a heating condition at 50-120 deg.C to industrially advantageously afford the objective compound expressed by formula II useful as an intermediate for production of medicine. The compound of formula II can also be isolated and purified by conventional method.

    PRODUCTION OF 3-(4-ETHOXY-2-AMINOPHENYL)PYRIDINE

    公开(公告)号:JPH02134364A

    公开(公告)日:1990-05-23

    申请号:JP28672388

    申请日:1988-11-15

    Applicant: KOWA CO

    Abstract: PURPOSE:To produce the title compound in high yield, industrially and advantageously by using one of 4-mesyloxy-2-nitrotoluene, 3-(2,4-dinitrophenyl)pyridine and 3-(4-ethoxyphenyl)pyridine as a raw material. CONSTITUTION:A compound shown by formula II is made into an ethyl ether compound, which is then reacted with pyrrolidine and N, N-dimethylformamide and then subjected to pyridine ring formation reaction to give a compound shown by formula V, which is reduced to give the title compound shown by formula I. A compound shown by formula VI is partially reduced to give a compound shown by formula VII, which is subjected to diazo hydrolysis reaction to give a compound shown by formula VIII. This compound is further ethyl etherified to give a compound shown by formula V, which is reduced to give the compound shown by formula I. A compound shown by formula IX is brominated to give a compound shown by formula X, which is further reacted with benzylamine to give a compound shown by formula XI, which is finally debenzylated to give the compound shown by formula I.

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