利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

37 条记录 (耗时 0.031 秒)

    Process for the preparation of lacosamide
    23.
    发明授权
    Process for the preparation of lacosamide 有权
    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。

    Process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine
    24.
    发明授权
    Process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine 有权
    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：

    Process for the preparation of doxifluridine
    26.
    发明申请
    Process for the preparation of doxifluridine 审中-公开
    制备杜伐菌苷的方法

    公开(公告)号：US20070073050A1

    公开(公告)日：2007-03-29

    申请号：US10576598

    申请日：2004-10-21

    申请人： Giorgio Bertolini ,  Marco Frigerio

    发明人： Giorgio Bertolini ,  Marco Frigerio

    IPC分类号： C07H19/12

    CPC分类号： C07H19/06 ,  C07H1/00

    摘要： A process is described for the preparation of doxifluridine of formula at high yields and with reduced formation of impurities, which comprises the reaction of coupling of a compound of formula (III) with a compound of formula (IV), as defined in the description, in the presence of a Lewis acid and in an inert organic solvent, characterized in that said Lewis acid is added at a temperature below 0° C.

    摘要翻译： 描述了以高产率制备式的多西菌定和减少杂质形成的方法，其包括式（III）化合物与式（IV）化合物如描述中所定义的反应， 在路易斯酸存在下和惰性有机溶剂中，其特征在于所述路易斯酸在低于0℃的温度下加入。

    Process for preparing (s)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetic acid
    27.
    发明申请
    Process for preparing (s)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetic acid 审中-公开
    制备四氢-α-（1-甲基乙基）-2-氧代-1（2h） - 嘧啶乙酸的方法

    公开(公告)号：US20050222184A1

    公开(公告)日：2005-10-06

    申请号：US10515964

    申请日：2003-05-28

    申请人： Giorgio Bertolini ,  Luca Feliciotti ,  Marco Frigerio ,  Massimo Losa

    发明人： Giorgio Bertolini ,  Luca Feliciotti ,  Marco Frigerio ,  Massimo Losa

    IPC分类号： C07B61/00 ,  C07D239/10 ,  A61K31/513 ,  C07D239/02

    CPC分类号： C07D239/10

    摘要： A process for preparing (S)-tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetic acid, an intermediate that is useful in the synthesis of HIV protease inhibitors such as, for example, those described in U.S. Pat. No. 5,914,332, is described. The process under consideration comprises the following steps:—L-valine is reacted with acrylonitrile;—the N-(2-cyanoethyl)-L-valine thus obtained is isolated and then reacted with an alkyl chloroformate;—the N-(2-cyanoethyl)-N-(alkoxycarbonyl)-L-valine thus obtained is hydro-genated in the presence of a hydrogenation catalyst, preferably rhodium;—the N-(3-aminopropyl)-N-(methoxycarbonyl)-L-valine thus obtained is cyclized to give the desired compound.

    摘要翻译： 制备（S） - 四氢-α-（1-甲基乙基）-2-氧代-1（2H） - 嘧啶乙酸的方法，该中间体可用于合成HIV蛋白酶抑制剂，例如所述的那些 在美国Pat。 第5,914,332号。 所考虑的方法包括以下步骤：将-L-缬氨酸与丙烯腈反应;分离得到的N-（2-氰基乙基）-L-缬氨酸，然后与氯甲酸烷基酯反应; - N-（2-氰基乙基） 氰基乙基）-N-（烷氧基羰基）-L-缬氨酸在氢化催化剂，优选铑的存在下氢化;由此获得的N-（3-氨基丙基）-N-（甲氧基羰基）-L-缬氨酸 环化得到所需化合物。