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1. 发明授权

US09410169B2 Process for producing chiral 1- substituted 2-piperidinols employing oxidoreductases 有权
标题翻译：使用氧化还原酶制备手性1-取代的2-哌啶醇的方法
公开(公告)号：US09410169B2
公开(公告)日：2016-08-09
申请号：US14406924
申请日：2012-06-18
申请人： Giorgio Bertolini , Paolo Magri′
发明人： Giorgio Bertolini , Paolo Magri′
IPC分类号： C12P13/00 , C12P17/12 , C12N9/02 , C12N9/04 , C07D211/42
CPC分类号： C12P17/12 , C07D211/42 , C12N9/0008 , Y02P20/52
摘要： The present invention relates to an enantioselective enzymatic process for the preparation of an optically active 3-hydroxypiperidinecarboxylic acid derivative.
摘要翻译：本发明涉及用于制备光学活性3-羟基哌啶羧酸衍生物的对映选择性酶法。

2. 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。

3. 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。

4. 发明申请

US20100226944A1 PROCESS FOR THE PREPARATION OF CONTROLLED-RELEASE SOLID FORMULATIONS CONTAINING OXCARBAZEPINE, AND FORMULATIONS OBTAINABLE BY SAID PROCESS 审中-公开
标题翻译：用于制备含有奥沙利铂的控制释放固体制剂的方法以及通过合适的方法获得的配方
公开(公告)号：US20100226944A1
公开(公告)日：2010-09-09
申请号：US12670273
申请日：2008-07-23
申请人： Giovanni Sanso' , Aldo Banfi , Giorgio Bertolini , Claudio Silva
发明人： Giovanni Sanso' , Aldo Banfi , Giorgio Bertolini , Claudio Silva
IPC分类号： A61K31/55 , A61P43/00 , A61K9/14
CPC分类号： A61K9/1694 , A61K9/009 , A61K9/146 , A61K9/1617 , A61K9/1623 , A61K9/1652 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/5031 , A61K9/5036 , A61K31/55
摘要： The present invention relates to a process for the preparation of controlled-release solid oral pharmaceutical formulations of oxcarbazepine, and the pharmaceutical formulations obtainable by said process.
摘要翻译：本发明涉及一种制备奥卡西平的控释固体口服药物制剂的方法，以及可通过所述方法获得的药物制剂。

5. 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：

6. 发明授权

US07534885B2 Process and intermediates for preparing emtricitabine 有权
标题翻译：制备恩曲他滨的方法和中间体
公开(公告)号：US07534885B2
公开(公告)日：2009-05-19
申请号：US10550718
申请日：2004-03-19
申请人： Giorgio Bertolini , Maurizio Deleo , Marco Frigerio , Massimo Losa , Maurizio Velati
发明人： Giorgio Bertolini , Maurizio Deleo , Marco Frigerio , Massimo Losa , Maurizio Velati
IPC分类号： C07D411/04 , A61K31/513 , A61K31/12
CPC分类号： C07D411/04
摘要： A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.
摘要翻译：公开了用于立曲达因选择性制备恩曲他滨的方法，其允许以良好的产率获得所需的产物，而不使用色谱技术。制备式（Ia）的恩曲他滨的方法的特征在于以成盐形式形成和分离式（XIa）的中间体化合物。恩曲他滨是一种已知的抗病毒药物。

7. 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。

8. 发明申请

US20060069272A1 Process for preparing 2,5-disubstituted 3-alkylthiophenes 审中-公开
标题翻译：制备2,5-二取代的3-烷基噻吩的方法
公开(公告)号：US20060069272A1
公开(公告)日：2006-03-30
申请号：US10530858
申请日：2003-10-13
申请人： Giorgio Bertolini , Marco Frigerio
发明人： Giorgio Bertolini , Marco Frigerio
IPC分类号： C07D333/16
CPC分类号： C07D333/22 , C07D333/08 , C07D333/16
摘要： The present invention relates to a process for preparing 2,5-disubstituted 3-alkyl-thiophenes and more particularly to a process for preparing them that comprises an acylation reaction in position 5 of 2-substituted 3-alkylthiophenes. This process does not need reagents which are difficult to handle and does not need anhydrous conditions or inert atmosphere. The resulting product is obtained in high purity.
摘要翻译：本发明涉及一种制备2,5-二取代的3-烷基 - 噻吩的方法，更具体地涉及一种制备它们的方法，其包括2-取代的3-烷基噻吩的5位的酰化反应。该方法不需要难以处理并且不需要无水条件或惰性气氛的试剂。得到的产物是高纯度的。

9. 发明授权

US06350873B2 Process for preparing 5′-acetylstavudine 失效
标题翻译：制备5'-乙酰胸苷的方法
公开(公告)号：US06350873B2
公开(公告)日：2002-02-26
申请号：US09834028
申请日：2001-04-12
申请人： Giorgio Bertolini , Marco Frigerio , Maurizio Velati , Luigi Petrucciani
发明人： Giorgio Bertolini , Marco Frigerio , Maurizio Velati , Luigi Petrucciani
IPC分类号： C07D23954
CPC分类号： C07H19/06
摘要： The present invention relates to a process for preparing 5′-acetylstavudine, an intermediate which is useful in the preparation of 2′,3′-didehydro-3′-deoxythymidine, an active principle with antiviral action which is commonly known as stavudine (D4T).
摘要翻译：本发明涉及一种制备5'-乙酰胸腺嘧啶的方法，该中间体可用于制备2'，3'-二脱氢-3'-脱氧胸苷，具有抗病毒作用的活性成分，其通常称为司他夫定（D4T ）。

10. 发明授权

US5827881A Diesters of carbonic acid endowed with antiviral and anti-inflammatory activity 失效
标题翻译：碳酸二酯具有抗病毒和抗炎活性
公开(公告)号：US5827881A
公开(公告)日：1998-10-27
申请号：US869043
申请日：1997-06-04
申请人： Alberto Sala , Giorgio Bertolini , Gianfranco Pavich , Fabrizio Marcucci , Gianni Gromo , Giuliana Porro
发明人： Alberto Sala , Giorgio Bertolini , Gianfranco Pavich , Fabrizio Marcucci , Gianni Gromo , Giuliana Porro
IPC分类号： A61K31/265 , A61K31/40 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61K31/445 , A61P29/00 , A61P31/12 , A61P37/06 , C07C219/16 , C07C219/20 , C07C219/22 , C07C219/24 , C07C219/32 , C07D207/08 , C07D207/12 , C07D211/22 , C07D213/30 , C07D295/088
CPC分类号： C07D207/08 , C07C219/16 , C07C219/22 , C07C219/24 , C07C219/32 , C07D211/22 , C07D295/088 , C07C2101/14
摘要： Diesters of carbonic acid disubstituted with primary, secondary or tertiary amine groups, pharmaceutically acceptable salts thereof, and their use as antiviral and inti-inflammatory agents.
摘要翻译：用伯胺，仲胺或叔胺二取代的碳酸二酯，其药学上可接受的盐，以及它们作为抗病毒和炎症介质的用途。

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