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21 条记录 (耗时 0.013 秒)

    METHYLTETRAZOLE SULFIDES AND SULFONES
    3.
    发明申请
    METHYLTETRAZOLE SULFIDES AND SULFONES 审中-公开
    甲基噻唑磺酸和硫磺

    公开(公告)号：WO2012098050A1

    公开(公告)日：2012-07-26

    申请号：PCT/EP2012/050471

    申请日：2012-01-13

    申请人： DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V. ,  LANGE, DE, Ben

    发明人： LANGE, DE, Ben

    IPC分类号： C07D413/12 ,  C07D419/12

    CPC分类号： C07D405/12 ,  C07D405/06 ,  C07D405/14 ,  C07D413/12 ,  C07D419/12

    摘要： The present invention relates to a process for the preparation of a 1-methyl-1 H -tetrazole-5-thio derivative comprising reaction of a halomethyl substrate with 1-methyl- H -tetrazole-5-thiol to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.

    摘要翻译： 本发明涉及1-甲基-1H-四唑-5-硫代衍生物的制备方法，其包括卤甲基底物与1-甲基-4-四唑-5-硫醇的反应，得到硫代醚化合物， 并将硫代醚化合物氧化成相应的砜。 在手性卤代甲基底物的情况下，所得手性二醇砜衍生物适合作为他汀类化合物的结构单元。

    STABALIZED STATIN-COMPRISING COMPOSITIONS
    4.
    发明申请
    STABALIZED STATIN-COMPRISING COMPOSITIONS 审中-公开

    公开(公告)号：WO2010066687A3

    公开(公告)日：2010-06-17

    申请号：PCT/EP2009/066546

    申请日：2009-12-07

    申请人： DSM IP ASSETS B.V. ,  LANGE, DE, Ben ,  UIL, DEN, Ronald

    发明人： LANGE, DE, Ben ,  UIL, DEN, Ronald

    IPC分类号： A61K9/16 ,  A61P3/06

    摘要： The present invention relates to a method for isolating a statin comprising spray drying a solution of said statin in an alcohol or precipitating said statin from said solution characterized in that two antioxidants are present in said solution or in that said antioxidants are added during said spray drying or during said precipitating. Furthermore there is provided a composition comprising a statin and 0.01% to 1% by weight of said composition of two antioxidants which are a carbohydrate, a carotenoid, a flavonoid, an isoflavonoid, a hydroxyacid, a phenol, a polyphenol, a sulphite salt, a terpene alcohol, thiourea, an unsaturated acid or a vitamin.

    PROCESS FOR THE PREPARATION OF A DIASTEREOMERICALLY ENRICHED COMPOUND
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF A DIASTEREOMERICALLY ENRICHED COMPOUND 审中-公开
    制备二异氰酸酯化合物的方法

    公开(公告)号：WO2006008171A1

    公开(公告)日：2006-01-26

    申请号：PCT/EP2005/007988

    申请日：2005-07-20

    申请人： DSM IP ASSETS B.V. ,  BROXTERMAN, Quirinus, Bernardus ,  LANGE, De Ben ,  ELSENBERG, Henricus, Leonardus, Marie ,  WEBER, Matthias

    发明人： BROXTERMAN, Quirinus, Bernardus ,  LANGE, De Ben ,  ELSENBERG, Henricus, Leonardus, Marie ,  WEBER, Matthias

    IPC分类号： C07C211/27

    CPC分类号： C07C209/28 ,  C07C2601/02 ,  C07C211/17 ,  C07C211/27 ,  C07C211/29

    摘要： The present invention relates to a process for the preparation of a diastereomerically enriched compound, wherein a first compound according to formula (I), is contacted with a second compound according to formula (II), to form a third compound according to formula (III), whereby the compound according to formula (III) is subsequently reduced and thereby converted into a compound according to formula (IV), in which formulas: R 1 = a cycloalkylgroup whereby R 1 # R 2 , R 2 = a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenylgroup, aryl group, cyclic or acyclic heteroalkylgroup or heteroarylgroup, R 3 = an alkyl group, R 4 = a substituted or unsubstituted: phenyl- or naphthyl-group, *= a chiral center. The invention furthermore relates to a diastereomerically enriched compound according to formula (IV) and its use in the preparation of pharmaceutical and agrochemically active compounds. The invention further relates to a process for the preparation of enantiomerically enriched compounds of formula (V), through hydrogenolysis of diastereomerically enriched compounds of formula (IV), wherein R 1 and R 2 have the meanings given above.

    摘要翻译： 本发明涉及一种制备非对映体富集的化合物的方法，其中根据式（I）的第一化合物与式（II）的第二化合物接触，以形成式（III）的第三化合物 ），由此将式（III）化合物随后还原，由此转化为式（Ⅳ）化合物，其中式

    METHOD FOR THE ISOLATION OF ATORVASTATIN
    10.
    发明申请
    METHOD FOR THE ISOLATION OF ATORVASTATIN 审中-公开
    分离ATORVASTATIN的方法

    公开(公告)号：WO2010066846A2

    公开(公告)日：2010-06-17

    申请号：PCT/EP2009066852

    申请日：2009-12-10

    申请人： DSM IP ASSETS BV ,  LANGE DE BEN ,  ELSENBERG HENRICUS LEONARDUS MARIE

    发明人： LANGE DE BEN ,  ELSENBERG HENRICUS LEONARDUS MARIE

    IPC分类号： C07D207/34

    CPC分类号： C07D207/34

    摘要： The present invention relates to a method for isolating atorvastatin comprising mixing at a temperature not exceeding 50ºC a solution of atorvastatin in methanol and/or ethanol and/or n-propanol with isopropanol and/or n-butanol and/or sec-butanol and/or tert-butanol and/or a linear or branched C5-alcohol and/or a linear or branched C6-alcohol and/or a linear or branched C7-alcohol, followed by isolating the precipitate thus obtained, optionally in the presence of one or more antioxidants.

    摘要翻译： 本发明涉及一种分离阿托伐他汀的方法，包括在不超过50℃的温度下混合阿托伐他汀在甲醇和/或乙醇和/或正丙醇中的溶液与异丙醇和/或正丁醇和/或仲丁醇和/ 或叔丁醇和/或直链或支链C 5 - 醇和/或直链或支链C 6 - 醇和/或直链或支链C 7 - 醇，然后任选地在一种或多种C 7 - 醇存在下分离由此获得的沉淀， 更多的抗氧化剂。