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    PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF
    2.
    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 preparing fexofenadine
    3.
    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。

    Process for the synthesis of tapentadol and intermediates thereof
    4.
    发明授权
    Process for the synthesis of tapentadol and intermediates thereof 有权
    合成他喷他多的方法及其中间体

    公开(公告)号：US08791287B2

    公开(公告)日：2014-07-29

    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： C07C69/76

    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。

    System for connecting juxtapposed sectional boards
    5.
    发明授权
    System for connecting juxtapposed sectional boards 失效
    用于连接并置分段板的系统

    公开(公告)号：US6065262A

    公开(公告)日：2000-05-23

    申请号：US110571

    申请日：1998-07-06

    申请人： Giuseppe Motta

    发明人： Giuseppe Motta

    IPC分类号： A47B96/20 ,  A47F5/08 ,  E04B2/74 ,  E04F19/06

    CPC分类号： E04B2/7416 ,  A47F5/0846 ,  E04B2002/7483 ,  Y10T403/7016

    摘要： System for connecting section boards, particularly panel-like elements having rectangular greater surfaces and horizontal greater sides to form partition walls includes two metal sections intended to connect a lower sectional board to an upper sectional board, one metal section being attached to the upper greater horizontal side of the lower sectional board and the other metal section being attached to the lower greater horizontal side of the upper sectional board, said metal sections being connected to each other by means of a tongue-and-groove joint and forming, once they are connected together, a recessed portion extending along the greater horizontal side of the sectional boards and intended to receive and hold therein a corresponding portion of an element or fixture intended to project or to hang from the partition wall.

    摘要翻译： 用于连接截面板的系统，特别是具有矩形较大表面和水平较大侧面的板状元件以形成分隔壁的系统包括用于将下部分板连接到上部分板的两个金属部分，一个金属部分连接到上部较大的水平面 所述下部分板的另一侧和另一个金属部分附接到上部分板的下部更大的水平侧，所述金属部分通过榫槽接头彼此连接并且一旦连接成形 一起是沿着分区板的较大水平侧延伸并且用于容纳和保持其中旨在从分隔壁突出或悬挂的元件或固定件的相应部分的凹部。

    Process for pressing materials
    6.
    发明授权
    Process for pressing materials 失效
    压制材料的工艺

    公开(公告)号：US6089147A

    公开(公告)日：2000-07-18

    申请号：US930290

    申请日：1997-09-30

    申请人： Lorenzo Rodriguez ,  Maurizio Cini ,  Cristina Cavallari ,  Giuseppe Motta

    发明人： Lorenzo Rodriguez ,  Maurizio Cini ,  Cristina Cavallari ,  Giuseppe Motta

    IPC分类号： B30B9/04 ,  B30B11/02 ,  B30B11/26 ,  B30B9/06

    CPC分类号： B30B11/227 ,  B30B11/022 ,  B30B11/26 ,  B30B9/04 ,  Y10S100/906

    摘要： A process is disclosed for pressing a material selected from materials of vegetable and animal origin. The process includes the steps of mechanically compressing the material of vegetable or animal origin while simultaneously vibrating the material at an ultrasonic frequency. The ultrasonic frequency going through the material modifies the material's internal state so as to considerably reduce resistance offered by the material to mechanical compression.

    摘要翻译： PCT No.PCT / IT97 / 00018 Sec。 371日期：1997年9月30日 102（e）1997年9月30日PCT PCT 1997年1月24日PCT公布。 出版物WO97 / 27994 日期1997年8月7日公开了一种用于压制选自植物和动物来源的材料的方法。 该方法包括以下步骤：机械地压缩植物或动物来源的材料，同时以超声频率振动材料。 穿过材料的超声波频率改变了材料的内部状态，从而显着降低了材料对机械压缩提供的阻力。

    Device for slowing the downwards travel of a vertically sliding wardrobe door
    7.
    发明授权
    Device for slowing the downwards travel of a vertically sliding wardrobe door 失效
    减慢垂直滑动衣柜门向下行驶的装置

    公开(公告)号：US5934776A

    公开(公告)日：1999-08-10

    申请号：US27628

    申请日：1998-02-23

    申请人： Giuseppe Motta

    发明人： Giuseppe Motta

    IPC分类号： E06B9/11 ,  E06B9/15

    CPC分类号： E06B9/115

    摘要： A device for slowing a downward movement of a sliding door of a wardrobe includes a free-wheel consisting of a driving portion and a driven portion. The driven portion is coaxially aligned with the driving portion and is provided with an external toothing. The device also includes a driving rope running through the free-wheel driving portion which is fastened at one end to the sliding door and at another end, by interposition of a tension spring, to a base of the wardrobe. Additionally a spring is arranged between the free-wheel driving and driven portions and is used to engage the two free-wheel portions during the downward movement of the sliding door and to disengage the two during upward movement of the sliding door. A centrifugal brake is coupled to a spindle which is provided with an external toothing cooperating with the external toothing of the free-wheel driven portion. The centrifugal brake is used to generate a resisting torque capable of braking the free-wheel driving and driven portions and slowing the downward movement of the sliding door.

    摘要翻译： 用于减慢衣柜的滑动门的向下运动的装置包括由驱动部分和被驱动部分组成的自由轮。 被驱动部分与驱动部分同轴对准并且设置有外齿。 该装置还包括一条驱动绳索，该驱动绳索穿过该自由轮驱动部分，该驱动绳索的一端固定在该滑动门上，另一端通过插入拉伸弹簧而固定在该衣柜的底座上。 此外，弹簧布置在自由轮驱动和被驱动部分之间，并且用于在滑动门的向下运动期间接合两个离合轮部分，并且在滑动门的向上运动期间使两者分离。 离心式制动器连接到主轴上，该心轴设有与辅助轮驱动部分的外齿配合的外齿。 离心式制动器用于产生能够制动自由轮驱动和被驱动部分并减缓滑动门的向下运动的阻力扭矩。

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

    公开(公告)号：US20110190504A1

    公开(公告)日：2011-08-04

    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： C07D211/34

    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 neutralisation 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。