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    PROCESS FOR THE PRODUCTION OF RALFINAMIDE SALTS SUBSTANTIALLY FREE FROM IMPURITIES HAVING GENOTOXIC EFFECTS
    8.
    发明申请
    PROCESS FOR THE PRODUCTION OF RALFINAMIDE SALTS SUBSTANTIALLY FREE FROM IMPURITIES HAVING GENOTOXIC EFFECTS 有权
    生产具有生殖毒性作用的重金属盐生产过程大量免费

    公开(公告)号：US20130039983A1

    公开(公告)日：2013-02-14

    申请号：US13643716

    申请日：2011-04-06

    申请人： Claudio Giordano ,  Erwin Waldvogel

    发明人： Claudio Giordano ,  Erwin Waldvogel

    IPC分类号： C07C303/32 ,  A61K9/28 ,  C07C309/04 ,  A61P25/28 ,  A61P25/08 ,  A61P25/04 ,  A61P25/06 ,  A61P25/24 ,  A61P25/00 ,  A61P29/00 ,  A61P15/00 ,  A61P13/00 ,  A61P3/00 ,  A61P1/00 ,  A61K31/205

    CPC分类号： C07C237/08 ,  A61K31/165 ,  C07C231/24

    摘要： The invention relates to a new process for the production and/or purification of the salt of the compound (S)-2-[4-(2-fluorobenzyloxy)benzylamino]propanamide, i.e. ralfinamide, or the respective R-enantiomer, with methanesulfonic acid in high yields and very high enantiomeric and chemical purity in the form of the crystalline anhydrous polymorph identified as form A, wherein said salt is substantially free from impurities having genotoxic effect, such as (C1-C5)alkanylmethanesulfonates, and residual solvents known as potential precursors thereof, such as (C1-C5)alkanols or esters thereof with lower alkanoic acids.The process foresees (i) production and/or crystallization of the salt, from water, acetone, an aliphatic ketone of 4-5 carbon, atoms or mixtures thereof with water, or (ii) slurring the solid salt with (a) water, (b) a mixture of water with acetone or an aliphatic ketone of 4-5 carbon atoms, (c) acetone, an aliphatic ketone of 4-5 carbon atoms or a mixture thereof, or (iii) exposure of the solid salt to air stream having high degree of relative humidity, and, when the obtained product consists as a whole or in part of crystalline hemihydrate pseudopolymorph form H crystals, converting said product into anhydrous form A crystals by submitting it to water removal.The crystalline hemihydrate pseudopolymorph form H of ralfinamide methanesulfonate, or its R-enantiomer, is a useful intermediate for obtaining the crystalline anhydrous polymorph A free from the above impurities having genotoxic effect and/or residual solvents known as precursors thereof, and exhibits a physicochemical profile conferring significant advantages in the design and development of solid dosage forms, in particular, of modified release formulations.

    摘要翻译： 本发明涉及一种用于生产和/或纯化化合物（S）-2- [4-（2-氟苄氧基）苄氨基]丙酰胺（即Ralfinamide）或相应的R-对映异构体与甲磺酸盐的新方法 酸的高产率和非常高的对映异构体和化学纯度，以结晶无水多晶型物的形式鉴定为形式A，其中所述盐基本上不含具有基因毒性作用的杂质，例如（C 1 -C 5）烷基甲磺酸盐，以及称为 其潜在的前体，例如（C1-C5）链烷醇或其与低级链烷酸的酯。 该方法预期（i）从水，丙酮，4-5碳原子或其混合物的水的脂族酮生成和/或结晶盐，或（ii）将固体盐与（a）水， （b）水与丙酮或4-5个碳原子的脂族酮的混合物，（c）丙酮，4-5个碳原子的脂肪族酮或其混合物，或（iii）将固体盐暴露于空气中 具有高相对湿度的流，并且当所得产物全部或部分由晶体半水合物假多晶型物形成H晶体时，通过将所述产物转移到除去水中而将所述产物转化为无水形式的A晶体。 Ralfinamide甲磺酸盐或其R-对映异构体的结晶半水合物假多晶型物形式H是获得不含上述具有遗传毒性作用的杂质的结晶无水多晶型物A和/或已知为其前体的残留溶剂的有用中间体，并且显示出物理化学特征 赋予固体剂型，特别是改性释放制剂的设计和开发中显着的优点。

    Process for the preparation of aryl-pyridinyl compounds
    9.
    发明授权
    Process for the preparation of aryl-pyridinyl compounds 有权
    芳基 - 吡啶基化合物的制备方法

    公开(公告)号：US06765097B1

    公开(公告)日：2004-07-20

    申请号：US10110685

    申请日：2002-04-11

    申请人： Claudio Giordano ,  Claudio Pozzoli ,  Fabio Benedetti

    发明人： Claudio Giordano ,  Claudio Pozzoli ,  Fabio Benedetti

    IPC分类号： C07D21346

    CPC分类号： C07D213/53 ,  C07D213/48 ,  C07D405/10

    摘要： A process is described for the preparation of arylpyridine compounds by aryl-aryl cross-coupling reactions between a halopyridine and an arylmagnesium halide carried out in the presence of a catalytic amount of a zinc salt and a catalytic amount of palladium. The zinc salt is preferably selected from ZnCl2, ZnBr2 and/or Zn(OAc)2, while the palladium is preferably used in the form of Pd(PPh3)4 or Pd(OAc)2 +4 PPh3. The reaction can also be carried out in the presence of bidentate phosphines, such as, for example, 1,3-bis(diphenylphosphine)propane or 1,4-bis(diphenylphosphine)-butane. It is thus possible to obtain molar yields higher than 97% (calculated relative to the halopyridine) and a catalyticity of more than 2000.

    摘要翻译： 描述了通过在催化量的锌盐和催化量的钯的存在下在卤代吡啶和卤化吡嗪之间的芳基 - 芳基交叉偶联反应制备芳基吡啶化合物的方法。 锌盐优选选自ZnCl 2，ZnBr 2和/或Zn（OAc）2，而钯优选以Pd（PPh 3）4或Pd（OAc）2 + 4 PPh 3的形式使用。 反应也可以在二齿膦存在下进行，例如1,3-双（二苯基膦）丙烷或1,4-双（二苯基膦） - 丁烷。 因此可以获得高于97％的摩尔收率（相对于卤代吡啶计算）和超过2000的催化剂。

    Process for the direct and regioselective functionalization in position 2 of phenothiazine
    10.
    发明授权
    Process for the direct and regioselective functionalization in position 2 of phenothiazine 失效
    吩噻嗪2位直接和区域选择性官能化方法

    公开(公告)号：US5362871A

    公开(公告)日：1994-11-08

    申请号：US833800

    申请日：1992-02-12

    申请人： Claudio Giordano ,  Maurizio Paiocchi ,  Paolo Cavalleri

    发明人： Claudio Giordano ,  Maurizio Paiocchi ,  Paolo Cavalleri

    IPC分类号： C07D279/22 ,  C07D279/20 ,  C07D279/30 ,  C07D279/32 ,  C07B45/06

    CPC分类号： C07D279/30 ,  C07D279/20

    摘要： A process for the direct and regioselective functionalization of phenothiazine which allows one to introduce an SH group in position 2, said process comprising the sulfination or sulfonation of the phenothiazine N-protected with an alkoxycarbonyl, an alkylsulfonyl or an arylsulfonyl group, the reduction of the produce obtained to give the N-protected 2-mercapto-phenothiazine, and the deprotection of the nitrogen atom. The thus-obtained 2-mercapto-phenothiazine is an important intermediate for the preparation of pharmacological active compounds.

    摘要翻译： 用于直接和区域选择性官能化吩噻嗪的方法，其允许在位置2引入SH基团，所述方法包括被烷氧基羰基，烷基磺酰基或芳基磺酰基N-保护的吩噻嗪的硫酸化或磺化， 得到N-保护的2-巯基吩噻嗪得到的产物和氮原子的去保护。 由此获得的2-巯基吩噻嗪是制备药理活性化合物的重要中间体。