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    PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF
    5.
    发明申请
    PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF 有权
    合成多巴多和其中间体的方法

    公开(公告)号：US20130178644A1

    公开(公告)日：2013-07-11

    申请号：US13807356

    申请日：2011-06-20

    申请人： Giuseppe Motta ,  Domenico Vergani ,  Giorgio Bertolini ,  Nicola Landoni

    发明人： Giuseppe Motta ,  Domenico Vergani ,  Giorgio Bertolini ,  Nicola Landoni

    IPC分类号： C07C229/38 ,  C07C217/62 ,  C07C217/72 ,  C07C213/08 ,  C07C225/16

    CPC分类号： C07C229/38 ,  C07B57/00 ,  C07B2200/07 ,  C07C213/00 ,  C07C213/06 ,  C07C213/08 ,  C07C213/10 ,  C07C217/62 ,  C07C217/72 ,  C07C219/22 ,  C07C221/00 ,  C07C225/16 ,  C07C215/54

    摘要： The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process.A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention.Still another object of the invention is represented by the crystalline forms I and II of the tapentadol free base.A further object of the present invention is the mixture of the crystalline forms I and II of the tapentadol free base.

    摘要翻译： 本发明的目的是合成无论是游离碱还是盐酸盐形式的他喷他多的新方法，其包括将酮（Ⅶ）烷基化以产生化合物（Ⅷ）的步骤，如图1所示 由于存在苄基作为氨基的取代基而具有高立体选择性。 令人惊讶地发现，该取代将酮 - 烯醇平衡转移到期望的对映异构体，并放大化合物（VII）中存在的立体中心的能力，以使有机金属化合物在羰基处的亲核加成反应成所需的立体异构体。 因此，这种置换可以在该步骤中获得相当大的产率增加，因此允许显着增加整个他喷他多合成过程的总产率。 本发明的另一个目的是通过本发明方法获得的固体形式的他喷他多游离碱构成。 本发明的另一个目的是由他喷他多游离碱的结晶形式I和II表示。 本发明的另一个目的是使用他喷他多游离碱的结晶形式I和II的混合物。

    PROCESS FOR THE PREPARATION OF LACOSAMIDE
    6.
    发明申请
    PROCESS FOR THE PREPARATION OF LACOSAMIDE 有权
    制备柠檬酰胺的方法

    公开(公告)号：US20130030216A1

    公开(公告)日：2013-01-31

    申请号：US13575152

    申请日：2010-12-22

    申请人： Alberto Bologna ,  Patrizia Castoldi ,  Domenico Vergani ,  Giorgio Bertolini

    发明人： Alberto Bologna ,  Patrizia Castoldi ,  Domenico Vergani ,  Giorgio Bertolini

    IPC分类号： C07C231/14 ,  C07C237/06

    CPC分类号： C07C237/22 ,  C07B2200/07 ,  C07C231/12 ,  C07C231/20 ,  C07C237/06

    摘要： A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

    摘要翻译： 描述了使用D，L-丝氨酸作为起始原料合成Lacosamide的新方法，其中羟基的甲基化反应使用廉价的碱如NaOH和廉价的烷基化剂进行，无毒和非致癌， 如对甲苯磺酸甲酯; 选择性水解乙酰胺后，将R对映异构体与赖氨酰胺的外消旋混合物分离，用有机溶剂中的手性酸（HX *）进行外消旋混合物的成盐，非对映异构体混合物的拆分，优选通过沉淀R对映异构体， 和随后的光学纯中间体的乙酰化。

    Benzoxazinone and benzothiazinone derivatives having cardiovascular activity
    7.
    发明授权
    Benzoxazinone and benzothiazinone derivatives having cardiovascular activity 失效
    具有心血管活性的苯并嗪酮和苯并噻嗪酮衍生物

    公开(公告)号：US5480882A

    公开(公告)日：1996-01-02

    申请号：US347217

    申请日：1994-11-23

    申请人： Alberto Sala ,  Roberto Barani ,  Francesca Benedini ,  Giorgio Bertolini ,  Giancarlo Dona ,  Gianni Gromo ,  Silvio Levi

    发明人： Alberto Sala ,  Roberto Barani ,  Francesca Benedini ,  Giorgio Bertolini ,  Giancarlo Dona ,  Gianni Gromo ,  Silvio Levi

    IPC分类号： A61K31/535 ,  A61K31/536 ,  A61K31/54 ,  A61K31/5415 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D265/22 ,  C07D279/08 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D265/22 ,  C07D279/08

    摘要： Compounds of formula I ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, methylene-dioxy or phenyl, which may be substituted by one or two groups independently selected from hydroxy, halogen, nitro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, COOR.sub.3, --CONR.sub.4 R.sub.5, ##STR2## --OCONR.sub.4 R.sub.5, --OCOR.sub.3, --NR.sub.4 R.sub.5, --OCOOR.sub.6, --NR.sub.3 COR.sub.7, --NR.sub.CONR.sub.4 R.sub.5, --N.dbd.CH--NR.sub.4 R.sub.5, NO.sub.2, CN, OH, SR.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 and R.sub.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, with the proviso that R.sub.1 and R.sub.2 cannot be hydrogen at the same time; X is oxygen or sulphur; Y represents a C.sub.2 -C.sub.6 alkylene chain or a C.sub.5 -C.sub.7 cycloalkylene group; and their pharmaceutically acceptable salts are provided and their use in pharmaceutical compositions which may be used in the treatment of cardiovascular diseases.

    摘要翻译： 式I的化合物其中R表示氢，C1-C6烷基，C5-C7环烷基，亚甲基 - 二氧基或苯基，其可以被一个或两个独立地选自羟基，卤素，硝基，C1 -C 1-6烷基或C 1 -C 6烷氧基; R1和R2独立地表示氢，COOR3，-CONR4R5，-OCONR4R5，-OCOR3，-NR4R5，-OCOOR6，-NR3COR7，-NRCONR4R5，-N = CH-NR4R5，NO2，CN，OH，SR3，其中R3 是氢或C1-C6烷基，R4和R5独立地是氢或C1-C6烷基，R6是C1-C6烷基，R7是氢，C1-C6烷基或C1-C6烷氧基，条件是R1和R2不能 同时是氢; X是氧或硫; Y表示C2-C6亚烷基链或C5-C7亚环烷基; 及其药学上可接受的盐，并且它们可用于可用于治疗心血管疾病的药物组合物中。

    Process for preparing fexofenadine
    10.
    发明授权
    Process for preparing fexofenadine 有权
    非索非那定制备方法

    公开(公告)号：US09403770B2

    公开(公告)日：2016-08-02

    申请号：US12374539

    申请日：2007-07-25

    申请人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

    发明人： Giorgio Bertolini ,  Maurizio Gallina ,  Giuseppe Motta ,  Domenico Vergani

    IPC分类号： C07D211/22

    CPC分类号： C07D211/22

    摘要： A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-α,α-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralization of the solution.

    摘要翻译： 描述了制备非索非那定的方法，其提供4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸 - 烷基酯在水溶液 水和任选的有机溶剂，在碱的存在下; 由此得到4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯乙酸的羧酸盐，然后在碱性环境中用氢气将其直接还原为羧酸盐 存在合适的氢化催化剂以得到通过溶液中和而沉淀的非索非那定的羧酸盐。