HYDROXY ACID COMPOUND OF SUBSTITUTED PHENYL ESTER, PREPARATION METHOD AND MEDICAL USE THEREOF
    22.
    发明公开
    HYDROXY ACID COMPOUND OF SUBSTITUTED PHENYL ESTER, PREPARATION METHOD AND MEDICAL USE THEREOF 有权
    HYDROXYSÄURENVERBINDUNGAUS EINEM SUBSTITUIERTEN PHENYLESTER,HERSTELLUNGSVERFAHREN UND MEDIZINISCHE VERWENDUNG

    公开(公告)号:EP2586768A1

    公开(公告)日:2013-05-01

    申请号:EP10853411.6

    申请日:2010-10-13

    CPC classification number: C07C59/48 C07C67/31 C07C67/32 C07C69/675

    Abstract: Hydroxy acid compound of substituted phenyl ester, preparation method and medical use thereof are provided. The title compound is shown in formula (I), Y = C 1-4 straight carbon chain. The compound can release 2, 6-diisopropylphenol rapidly under the action of enzymes in vivo, which has sedative, hypnotic and/or anesthetic effect. By protecting the hydroxyl group of 2, 6-diisopropylphenol in compound of formula (I), the first-pass metabolic activity of 2, 6-diisopropylphenol is reduced, so that the synthetic compound can be used for sedation, hypnosis, and/or anesthesia.

    Abstract translation: 提供取代苯基酯的羟基酸化合物,其制备方法和医疗用途。 标题化合物如式(I)所示,Y = C 1-4直链碳链。 该化合物可在体内酶的作用下快速释放2,6-二异丙基苯酚,具有镇静,催眠和/或麻醉作用。 通过保护式(I)化合物中2,6-二异丙基苯酚的羟基,2,6-二异丙基苯酚的首过代谢活性降低,合成化合物可用于镇静,催眠和/或 麻醉。

    ROSUVASTATIN CALCIUM INTERMEDIATE AND PREPARATION METHOD THEREOF
    24.
    发明公开
    ROSUVASTATIN CALCIUM INTERMEDIATE AND PREPARATION METHOD THEREOF 有权
    ROSUVASTATIN钙中间体及其制备方法

    公开(公告)号:EP2557084A1

    公开(公告)日:2013-02-13

    申请号:EP10849287.7

    申请日:2010-07-28

    Abstract: A rosuvastatin calcium intermediate as shown by Formula I is prepared as follow: a) subjecting chloroethylene, magnesium and R-epoxy chloropropane to Grignard reaction, b) adding sodium cyanide for nucleophilic substitution reaction, c) adding alcohol for alcoholysis reaction, d) adding alkaline solvent for hydroxyl protection, e) subjecting the mixture to oxidation reaction, f) adding triphenyl phosphorus and subjecting to Wittig reaction in the presence of alkali to obtain the compound of formula I. The method has moderate reaction conditions, is convenient and stable and can be applied to industrial production.

    Abstract translation: 式I所示的瑞舒伐他汀钙中间体如下制备:a)使氯乙烯,镁和R-环氧氯丙烷进行格氏反应,b)加入氰化钠进行亲核取代反应,c)加入醇进行醇解反应,d)加入 e)将混合物进行氧化反应,f)加入三苯基磷并在碱存在下进行维g希反应,得到式I化合物。该方法反应条件温和,方便稳定, 可以应用于工业生产。

    Process for the preparation of an intermediate for azoxystrobin
    28.
    发明公开
    Process for the preparation of an intermediate for azoxystrobin 有权
    Verfahren zur Herstellung eines ZwischenproduktsfürAzoxystrobin

    公开(公告)号:EP2308825A1

    公开(公告)日:2011-04-13

    申请号:EP10013918.7

    申请日:2006-04-13

    CPC classification number: C07C69/734 C07C67/31 C07C67/327 Y02P20/55

    Abstract: The present invention relates to a process for preparing a compound of formula (IV)

    where W is the methyl ( E )-2-(3-methoxy)acrylate group, which comprises the steps of: (i) reacting the compound of formula (IV) where W is the methyl 2-(3,3-dimethoxy)propanoate group with a reagent that will protect the hydroxyl group of that compound from reaction during subsequent demethanolysis; (ii) eliminating methanol from the hydroxyl-protected compound formed in step (i); and (iii) removing the hydroxyl-protecting group formed in step (i) to form a compound of formula (IV) where W is the methyl ( E )-2-(3-methoxy)acrylate group.

    Abstract translation: 本发明涉及制备其中W是(E)-2-(3-甲氧基)丙烯酸甲酯基团的式(Ⅳ)化合物的方法,该方法包括以下步骤:(ⅰ)使式 IV)其中W是2-(3,3-二甲氧基)丙酸甲酯基团,其具有将在随后的脱甲硅烷溶解期间保护该化合物的羟基反应的试剂; (ii)从步骤(i)中形成的羟基保护的化合物中除去甲醇; 和(iii)除去步骤(i)中形成的羟基保护基以形成其中W是甲基(E)-2-(3-甲氧基)丙烯酸酯基团的式(IV)化合物。

    METHOD FOR PRODUCING PHENOLIC COMPOUND
    29.
    发明公开
    METHOD FOR PRODUCING PHENOLIC COMPOUND 有权
    一种用于生产酚类化合物

    公开(公告)号:EP2300414A1

    公开(公告)日:2011-03-30

    申请号:EP09767900.5

    申请日:2009-06-22

    CPC classification number: C07C67/03 C07C67/31 C07C69/84

    Abstract: A method is provided for producing an ester-substituted phenol product stream from an ester-substituted diaryl carbonate manufacturing waste stream. The method includes the steps of obtaining a waste stream containing an ester-substituted diaryl carbonate from an ester-substituted diaryl carbonate manufacturing facility and creating a reaction mixture by combining the waste stream with a solvent and with a transesterification catalyst. The reaction mixture is maintained at a reaction pressure at or below atmospheric pressure, and at a reaction temperature for a period of time sufficient to produce ester-substituted phenol by solvolysis of the ester-substituted diaryl carbonate. Ester-substituted phenol is removed from the reaction mixtures in an ester-substituted phenol stream. The solvent, the reaction temperature, and the reaction time are selected in combination such that less than 1,000 ppm of acid-substituted phenol is present in the ester-substituted phenol stream.

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