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1. 发明申请

US20130030216A1 PROCESS FOR THE PREPARATION OF LACOSAMIDE 有权
标题翻译：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。

2. 发明授权

US08796488B2 Process for the preparation of lacosamide 有权
标题翻译：制备漆酶的方法
公开(公告)号：US08796488B2
公开(公告)日：2014-08-05
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： C07C233/06 , C07C231/14 , C07C231/20 , C07C231/12 , C07C237/22 , 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。

3. 发明申请

US20060199959A1 Process for preparing 2',3'-didehydro-2'3'-dideoxynucleosides and 2',3'-dideoxynucleosides 审中-公开
标题翻译：制备2'，3'-二脱水-2,3'-二脱氧核苷和2'，3'-二脱氧核苷的方法
公开(公告)号：US20060199959A1
公开(公告)日：2006-09-07
申请号：US10567696
申请日：2004-07-29
申请人： Giorgio Bertolini , Patrizia Castoldi , Mauricio Deleo , Marco Frigerio , Maurizio Velati
发明人： Giorgio Bertolini , Patrizia Castoldi , Mauricio Deleo , Marco Frigerio , Maurizio Velati
IPC分类号： C07F9/6512
CPC分类号： C07H19/06 , C07H19/16 , Y02P20/55
摘要： A process for preparing 2′,3′-didehydro-2′,3′-dideoxynucleosides and 2′,3′-dideoxynucleosides is described, which comprises the reductive elimination reaction of a compound of formula in which X, Y, P′ is H or a protecting group and B is a natural or modified, optionally substituted purine or pyrimidine base or a five- or six-membered monocyclic or eleven- or twelve-membered bicyclic, optionally substituted heterocyclic system containing at least one nitrogen atom, by reaction with zinc metal and a suitable activating agent, characterized in that the divalent zinc is removed by precipitation, from an organic phase, of the corresponding zinc sulfide, by adding a solution of a mineral sulfide to the organic phase.
摘要翻译：描述了制备2'，3'-二脱氢-2'，3'-双脱氧核苷和2'，3'-二脱氧核苷的方法，其包括式X化合物的还原消除反应，其中X，Y，P' H或保护基，B是通过反应的天然或修饰的任选取代的嘌呤或嘧啶碱基或五元或六元单环或十一元或十二元双环，任选取代的含有至少一个氮原子的杂环体系其中锌金属和合适的活化剂，其特征在于，通过向有机相中加入无机硫化物溶液，通过从有机相中沉淀出相应的硫化锌来除去二价锌。

4. 发明授权

US08729308B2 Process for the preparation of tapentadol and intermediates thereof 有权
标题翻译：制备他喷他多的方法及其中间体
公开(公告)号：US08729308B2
公开(公告)日：2014-05-20
申请号：US13512989
申请日：2010-11-30
申请人： Giuseppe Motta , Domenico Vergani , Giorgio Bertolini
发明人： Giuseppe Motta , Domenico Vergani , Giorgio Bertolini
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。

5. 发明申请

US20130178644A1 PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF 有权
标题翻译：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。

6. 发明授权

US09403770B2 Process for preparing fexofenadine 有权
标题翻译：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。

7. 发明授权

US08791287B2 Process for the synthesis of tapentadol and intermediates thereof 有权
标题翻译：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。

8. 发明申请

US20100105942A1 Process for the Synthesis of Aryloxypropylamine and Heteroaryloxypropylamine 有权
标题翻译：合成丙烯酰胺和异丙氧基丙胺的方法
公开(公告)号：US20100105942A1
公开(公告)日：2010-04-29
申请号：US12444710
申请日：2007-10-04
申请人： Giorgio Bertolini , Barbara Verzola , Domenico Vergani
发明人： Giorgio Bertolini , Barbara Verzola , Domenico Vergani
IPC分类号： C07C211/27 , C07C271/14 , C07C317/14
CPC分类号： C07C303/40 , C07C213/02 , C07C303/38 , C07C311/16 , C07C217/48
摘要： The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:
摘要翻译：本发明涉及一种用于合成式I的芳氧基丙胺和杂芳氧基丙胺的方法：其中：A是芳基或杂芳基，其中芳基优选为任选取代的苯基，选自苄基和甲苯基，杂芳基优选为噻吩基; Y是芳基，优选苯基，取代的苯基或萘基，其中取代的苯基优选选自甲酰基，三卤代甲基甲酰基和烷氧基酰基，从式II的合适的氨基醇开始：

9. 发明授权

US08367868B2 Process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine 有权
标题翻译：芳氧基丙胺和杂芳氧基丙胺的合成方法
公开(公告)号：US08367868B2
公开(公告)日：2013-02-05
申请号：US12444710
申请日：2007-10-04
申请人： Giorgio Bertolini , Barbara Verzola , Domenico Vergani
发明人： Giorgio Bertolini , Barbara Verzola , Domenico Vergani
IPC分类号： C07C209/14
CPC分类号： C07C303/40 , C07C213/02 , C07C303/38 , C07C311/16 , C07C217/48
摘要： The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:
摘要翻译：本发明涉及一种用于合成式I的芳氧基丙胺和杂芳氧基丙胺的方法：其中：A是芳基或杂芳基，其中芳基优选为任选取代的苯基，选自苄基和甲苯基，杂芳基优选为噻吩基; Y是芳基，优选苯基，取代的苯基或萘基，其中取代的苯基优选选自甲酰基，三卤代甲基甲酰基和烷氧基酰基，从式II的合适的氨基醇开始：

10. 发明申请

US20120232306A1 PROCESS FOR THE PREPARATION OF TAPENTADOL AND INTERMEDIATES THEREOF 有权
标题翻译：制备他哌多醇及其中间体的方法
公开(公告)号：US20120232306A1
公开(公告)日：2012-09-13
申请号：US13512989
申请日：2010-11-30
申请人： Giuseppe Motta , Domenico Vergani , Giorgio Bertolini
发明人： Giuseppe Motta , Domenico Vergani , Giorgio Bertolini
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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