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公开(公告)号：US09403770B2
公开(公告)日：2016-08-02
申请号：US12374539
申请日：2007-07-25
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。
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公开(公告)号：US20110190504A1
公开(公告)日：2011-08-04
申请号：US12374539
申请日：2007-07-25
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。
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公开(公告)号：US08729308B2
公开(公告)日：2014-05-20
申请号：US13512989
申请日：2010-11-30
IPC分类号： C07C211/00 , C07C221/00 , C07C225/00 , C07C223/00
CPC分类号： C07C221/00 , C07B2200/07 , C07C209/68 , C07C213/00 , C07C225/16 , C07C233/43 , C07C245/20 , C07C211/49 , C07C215/68
摘要： The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below using the (2R,3R)—O,O′-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.
摘要翻译： 本发明涉及用于合成外用混合物（Ⅴ）的定量分辨率以获得（S）-3-（二甲基氨基）-2-甲基-1-（3-硝基苯基） - 丙-1-酮（VII），使用（2R，3R）-O，O-二苯甲酰基酒石酸手性酸，其中所述分辨率是定量的。 本发明还涉及一些新的合成过程的中间化合物。
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公开(公告)号：US20130178644A1
公开(公告)日：2013-07-11
申请号：US13807356
申请日：2011-06-20
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。
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公开(公告)号：US08791287B2
公开(公告)日：2014-07-29
申请号：US13807356
申请日：2011-06-20
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。
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公开(公告)号：US20120232306A1
公开(公告)日：2012-09-13
申请号：US13512989
申请日：2010-11-30
IPC分类号： C07C209/78 , C07C225/16 , C07C233/43 , C07C209/68 , C07C69/63
CPC分类号： C07C221/00 , C07B2200/07 , C07C209/68 , C07C213/00 , C07C225/16 , C07C233/43 , C07C245/20 , C07C211/49 , C07C215/68
摘要： The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below using the (2R,3R)—O,O′-dibenzoyltartaric chiral acid wherein said resolution is quantitative.The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.
摘要翻译： 本发明涉及用于合成外用混合物（Ⅴ）的定量分辨率以获得（S）-3-（二甲基氨基）-2-甲基-1-（3-硝基苯基） - 丙-1-酮（VII），使用（2R，3R）-O，O-二苯甲酰基酒石酸手性酸，其中所述分辨率是定量的。 本发明还涉及一些新的合成过程的中间化合物。
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公开(公告)号：US20100016599A1
公开(公告)日：2010-01-21
申请号：US12374688
申请日：2007-07-25
申请人： Giuseppe Motta , Domenico Vergani
发明人： Giuseppe Motta , Domenico Vergani
IPC分类号： C07D211/34 , C07C69/76
CPC分类号： C07D211/22 , C07C67/52 , C07C69/738
摘要： A process for preparing fexofenadine is described that includes the purification of 4-[4-chloro-1-oxobutyl]-2,2-dimethylphenyl acetic acid alkyl ester by means of suspension in a hydrocarbon, preferably n-heptane. The compound thus obtained is dissolved in a suitable solvent and condensed with azacyclanol to give the compound shown below where R is an alkyl radical, which is then hydrolysed and reduced to give fexofenadine.
摘要翻译： 描述了一种制备非索非那定的方法，其包括通过在烃，优选正庚烷中的悬浮液纯化4- [4-氯-1-氧代丁基] -2,2-二甲基苯基乙酸烷基酯。 将由此获得的化合物溶于合适的溶剂中并与氮杂环丙烷缩合，得到下文所示的化合物，其中R是烷基，然后将其水解并还原得到非索非那定。
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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
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。
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公开(公告)号：US6089147A
公开(公告)日：2000-07-18
申请号：US930290
申请日：1997-09-30
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。
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10.发明授权
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
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。
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