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    PROCESS FOR THE PREPARATION OF ARYLOXYPROPYLAMINES
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF ARYLOXYPROPYLAMINES 审中-公开
    制备芳基丙烯酰胺的方法

    公开(公告)号：US20070270483A1

    公开(公告)日：2007-11-22

    申请号：US11749977

    申请日：2007-05-17

    申请人： Simone MANTEGAZZA ,  Gabriele RAZZETTI ,  Marcello RASPARINI ,  Roberto ROSSI ,  Pietro ALLEGRINI

    发明人： Simone MANTEGAZZA ,  Gabriele RAZZETTI ,  Marcello RASPARINI ,  Roberto ROSSI ,  Pietro ALLEGRINI

    IPC分类号： A61K31/381 ,  C07D333/22

    CPC分类号： C07C213/08 ,  Y02P20/55

    摘要： A process for preparation of a compound of formula (I), or a salt thereof, both as individual isomer and as mixtures thereof, wherein each of A and B is independently aryl or heteroaryl optionally substituted with 1 to 4 substituents; and R and R1, which can be the same or different, are hydrogen, C1-C6 alkyl or an amino-protecting group; comprising the reaction of a compound (II) wherein A and B are as defined above, with a compound (III) wherein each of R and R1 is independently C1-C6 alkyl or an amino-protecting group; and X is a leaving group; in the presence of a basic agent; and, if desired the conversion of a compound (I) to another compound (I); and/or, if desired, the separation of an isomeric mixture of a compound (I) into the individual isomers; and/or, if desired, the conversion of a compound (I) to a salt thereof.

    摘要翻译： 制备式（I）化合物或其盐作为单独异构体及其混合物的方法，其中A和B各自独立地为任选被1至4个取代基取代的芳基或杂芳基; R 1和R 2可以相同或不同，为氢，C 1 -C 6烷基或氨基保护基 ; 包括其中A和B如上定义的化合物（II）与化合物（III）的反应，其中R和R 1各自独立地为C 1〜 C 6烷基或氨基保护基; X为离去群; 在一个基本代理人的面前; 并且如果需要，化合物（I）转化为另一化合物（I）; 和/或如果需要，将化合物（I）的异构体混合物分离成单独的异构体; 和/或如果需要，化合物（I）转化为其盐。

    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS 失效
    制备吡啶化合物的方法

    公开(公告)号：US20070249662A1

    公开(公告)日：2007-10-25

    申请号：US11737852

    申请日：2007-04-20

    申请人： Pietro ALLEGRINI ,  Marcello Rasparini ,  Gabriele Razzetti ,  Roberto Rossi ,  Gianpiero Ventimiglia

    发明人： Pietro ALLEGRINI ,  Marcello Rasparini ,  Gabriele Razzetti ,  Roberto Rossi ,  Gianpiero Ventimiglia

    IPC分类号： A61K31/4439 ,  A61K31/4745 ,  C07D471/02 ,  C07D403/02

    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; andeach 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-CR 8 - 或-N-; 每个R 1，R 2，R 3，R 4，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C 1 -C 6烷基; 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与它们所连接的氮原子一起 形成饱和杂环; 并且每个R 5，R 6，R 7，R 8和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C 1 -C 6烷基; 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烷氧基 - 羰基和恶唑-2（C 1 -C 6） - 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 ENTACAPONE
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF ENTACAPONE 失效
    制备ENTACAPONE的方法

    公开(公告)号：US20080146829A1

    公开(公告)日：2008-06-19

    申请号：US11958778

    申请日：2007-12-18

    申请人： Simone MANTEGAZZA ,  Pietro ALLEGRINI ,  Gabriele RAZZETTI

    发明人： Simone MANTEGAZZA ,  Pietro ALLEGRINI ,  Gabriele RAZZETTI

    IPC分类号： C07C255/23

    CPC分类号： C07C253/30 ,  C07C255/41

    摘要： A process for the preparation of entacapone, in particular as the polymorphic form A, comprising the preparation of a compound of formula (V), as herein defined, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), as herein defined, in the presence of a strong basic agent; the dealkylation of said compound of formula (V) to obtain entacapone and the crystallization thereof to the polymorphic form A.

    摘要翻译： 恩替卡朋的制备方法，特别是多晶型A，其包括通过N，N-二乙基 - 氰基 - 乙酰胺与式（III）化合物的缩合制备如本文定义的式（Ⅴ）化合物 IV），如本文所定义的，在强碱性剂的存在下; 所述式（V）化合物的脱烷基化以获得恩他卡朋，并将其结晶化为多晶型A.

    PROCESS FOR THE PURIFICATION OF RUFINAMIDE
    10.
    发明申请
    PROCESS FOR THE PURIFICATION OF RUFINAMIDE 有权
    净化呋喃胺的方法

    公开(公告)号：US20120277443A1

    公开(公告)日：2012-11-01

    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： C07D249/04

    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; andc) 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。