利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

61 条记录 (耗时 0.02 秒)

    Process for the purification of rufinamide
    1.
    发明授权
    Process for the purification of rufinamide 有权
    Rufinamide净化方法

    公开(公告)号：US08461190B2

    公开(公告)日：2013-06-11

    申请号：US13451651

    申请日：2012-04-20

    申请人： Pietro Allegrini ,  Dario Pastorello ,  Gabriele Razzetti

    发明人： Pietro Allegrini ,  Dario Pastorello ,  Gabriele Razzetti

    IPC分类号： A61K31/41 ,  C07D249/00

    CPC分类号： C07D249/04

    摘要： A process for purifying Rufinamide, comprising: a) providing a dispersion of crude 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide in a solvent mixture containing at least a carboxylic acid, and dissolving it; b) slowly cooling the solution to precipitate Rufinamide crystalline form A; and c) recovering the solid.

    摘要翻译： 一种用于纯化Rufinamide的方法，包括：a）提供粗制的1 - [（2,6-二氟苯基）甲基] -1H-1,2,3-三唑-4-甲酰胺在含有至少一种羧酸 酸，并溶解; b）缓慢冷却溶液以沉淀Ruformamide结晶形式A; 和c）回收固体。

    Process for the Preparation of (S)(+)-3-(Aminomethyl)-5-Methylhexanoic Acid
    2.
    发明申请
    Process for the Preparation of (S)(+)-3-(Aminomethyl)-5-Methylhexanoic Acid 审中-公开
    （S）（+） - 3-（氨基甲基）-5-甲基己酸的制备方法

    公开(公告)号：US20090143615A1

    公开(公告)日：2009-06-04

    申请号：US12327191

    申请日：2008-12-03

    申请人： Pietro Allegrini ,  Simone Mantegazza ,  Dario Pastorello ,  Gabriele Razzetti

    发明人： Pietro Allegrini ,  Simone Mantegazza ,  Dario Pastorello ,  Gabriele Razzetti

    IPC分类号： C07C229/04 ,  C07C243/10

    CPC分类号： C07C227/34 ,  C07C229/08 ,  C07C243/28

    摘要： A process for the preparation of a compound of formula (I), comprising:a) the reaction of a compound of formula (II) with hydrazine to obtain a compound of formula (III), b) the conversion of a compound of formula (III) by rearrangement via formation of nitrene/isocyanate, in a solvent of formula R1—OH, wherein R1 is as herein defined, to obtain a compound of formula (IV); c) the enantiomeric enrichment of a compound of formula (IV) to obtain the enantiomer (S) of a compound of formula (V) d) the hydrolysis of a compound of formula (V).

    摘要翻译： 一种制备式（I）化合物的方法，包括：a）式（II）化合物与肼的反应得到式（III）化合物，b）式（I）化合物 III）通过在式R 1 -OH的溶剂中通过形成硝酸/异氰酸酯重排，其中R 1如本文所定义，以获得式（IV）的化合物; c）式（Ⅳ）化合物的对映异构体富集，得到式（Ⅴ）化合物的对映异构体（S）; d）式（Ⅴ）化合物的水解。

    Process for the synthesis of pregabalin
    3.
    发明授权
    Process for the synthesis of pregabalin 失效
    合成普瑞巴林的方法

    公开(公告)号：US08063244B2

    公开(公告)日：2011-11-22

    申请号：US12770044

    申请日：2010-04-29

    申请人： Gabriele Razzetti ,  Pietro Allegrini ,  Dario Pastorello

    发明人： Gabriele Razzetti ,  Pietro Allegrini ,  Dario Pastorello

    IPC分类号： C07C229/00 ,  C07B53/00

    CPC分类号： C07C229/08 ,  C07C227/04

    摘要： A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2  (III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.

    摘要翻译： 公开了制备式（I）化合物的方法，其包括：a）在存在下使式（II）化合物与式（III）的叠氮化锌（N 3）2（III） 的式R 1 -OH的溶剂，其中R 1在本文中定义，以获得式（IV）的化合物，b）其转化为式（V）的化合物; c）其对映体富集以获得式（VI）的（S）对映异构体; 和d）其水解。

    Synthesis of intermediates for the preparation of pramipexol
    8.
    发明授权
    Synthesis of intermediates for the preparation of pramipexol 失效
    用于制备普拉克索的中间体的合成

    公开(公告)号：US07662610B2

    公开(公告)日：2010-02-16

    申请号：US11622259

    申请日：2007-01-11

    申请人： Sergio Riva ,  Paola Fassi ,  Michele Scarpellini ,  Pietro Allegrini ,  Gabriele Razzetti

    发明人： Sergio Riva ,  Paola Fassi ,  Michele Scarpellini ,  Pietro Allegrini ,  Gabriele Razzetti

    IPC分类号： C12P41/00

    CPC分类号： C12P17/14 ,  C07D277/82 ,  C12P41/005

    摘要： A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R,S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; (the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.

    摘要翻译： 制备式（I）的酸作为单个（R）对映异构体或（S）的方法或其盐，其中R是被保护的氨基; 并且星号*表示立体碳原子，包括使式（II）的酯作为（R，S）对映体或其盐的混合物接触，其中R 1是直链或支链的C 1 -C 6烷基，任选被苯基 ; （上文定义的星号*和R）与来自南极念珠菌的脂肪酶在有效获得包含式（I）的酸的混合物作为个体（R）对映异构体的条件下，和式（II）的酯， 作为个体（S）对映体; 随后水解后者以获得式（I）的酸作为单独的（S）对映异构体; 如果需要，将式（I）的酸作为（R）或（S）对映异构体转化为其盐。

    Process for the preparation of pyridine compounds
    9.
    发明授权
    Process for the preparation of pyridine compounds 失效
    吡啶化合物的制备方法

    公开(公告)号：US07605268B2

    公开(公告)日：2009-10-20

    申请号：US11737852

    申请日：2007-04-20

    申请人： Pietro Allegrini ,  Marcello Rasparini ,  Gabriele Razzetti ,  Roberto Rossi ,  Gianpiero Ventimigla

    发明人： Pietro Allegrini ,  Marcello Rasparini ,  Gabriele Razzetti ,  Roberto Rossi ,  Gianpiero Ventimigla

    IPC分类号： C07D401/12

    CPC分类号： C07D471/04 ,  C07D401/12

    摘要： A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.

    摘要翻译： 制备式（I）化合物的方法，均为异构体混合物和各异构体，其中Q为-CR8-或-N-; 每个R 1，R 2，R 3，R 4独立地选自氢，卤素，羟基; 硝基 任选被羟基取代的C 1 -C 6烷基; 烷硫基C1-C6; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N（RaRb），其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们连接的氮原子一起形成饱和杂环; 并且每个R 5，R 6，R 7，R 8独立地选自氢，卤素，羟基; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C1-C6; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基，C 1 -C 6烷氧羰基和恶唑-2-基; 包括在催化剂存在下，如果需要在有机溶剂中将式（Ⅳ）化合物转化为所述式（Ⅳ）化合物。

    Process for the preparation of adapalene
    10.
    发明授权
    Process for the preparation of adapalene 失效
    阿达帕林制备方法

    公开(公告)号：US07345189B2

    公开(公告)日：2008-03-18

    申请号：US11392909

    申请日：2006-03-30

    申请人： Graziano Castaldi ,  Pietro Allegrini ,  Gabriele Razzetti ,  Mauro Ercoli

    发明人： Graziano Castaldi ,  Pietro Allegrini ,  Gabriele Razzetti ,  Mauro Ercoli

    IPC分类号： C07C69/76

    CPC分类号： C07C51/412 ,  C07C51/02 ,  C07C67/343 ,  C07C2603/74 ,  C07C65/26 ,  C07C69/94

    摘要： A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

    摘要翻译： 制备式（I）化合物或其盐的方法，其中R为H，C 1 -C 8烷基，芳基或芳基-C C 1 -C 8烷基; 包括其中R 1和R 2独立地是氢，C 1 -C 8的式（II）化合物之间的反应 烷基，芳基，芳基-C 1 -C 8烷基或R 1和R 2