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    Process for the preparation of tolterodine
    1.
    发明授权
    Process for the preparation of tolterodine 失效
    制备托特罗定的方法

    公开(公告)号：US07335793B2

    公开(公告)日：2008-02-26

    申请号：US11356953

    申请日：2006-02-21

    申请人： Gabriele Razzetti ,  Simone Mantegazza ,  Roberto Rossi ,  Pietro Allegrini

    发明人： Gabriele Razzetti ,  Simone Mantegazza ,  Roberto Rossi ,  Pietro Allegrini

    IPC分类号： C07C211/00 ,  C09B11/02

    CPC分类号： C07C215/54 ,  C07C69/736 ,  C07C217/18 ,  C07C233/18

    摘要： A novel process prepares tolterodine, i.e. (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine, in the racemic form, as well as intermediates useful for its preparation. Tolterodine free base may be prepared by reacting diisopropyl-(3-phenyl-3-p-tolyloxy-propyl)-amine and 60% aqueous sulfuric acid for three hours under stirring at room temperature. The reaction mixture is then poured over ice/water and then alkalized with 50% NaOH.

    摘要翻译： 一种新颖的方法制备托特罗定，即外消旋形式的（R）-N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基丙胺，以及可用于其制备的中间体。 通过二异丙基 - （3-苯基-3-对甲氧基 - 丙基） - 胺和60％硫酸水溶液在室温搅拌下反应3小时可以制备托特罗定游离碱。 然后将反应混合物倒入冰/水中，然后用50％NaOH碱化。

    Process for the preparation of pyridine compounds
    6.
    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 ZILEUTON
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF ZILEUTON 审中-公开
    制备ZILEUTON的方法

    公开(公告)号：US20090286996A1

    公开(公告)日：2009-11-19

    申请号：US12423122

    申请日：2009-04-14

    申请人： Emanuele ATTOLINA ,  Gianmaria Dell'Anna ,  Roberto Rossi ,  Pietro Allegrini ,  Gabriele Razzetti

    发明人： Emanuele ATTOLINA ,  Gianmaria Dell'Anna ,  Roberto Rossi ,  Pietro Allegrini ,  Gabriele Razzetti

    IPC分类号： C07D333/58 ,  C07D333/60 ,  C07F7/10

    CPC分类号： C07D333/56 ,  C07D333/58 ,  C07F7/1804 ,  Y02P20/55

    摘要： Process for preparing a compound of formula (I), or a salt thereof, comprising reacting of a compound of formula (II) wherein X and R are as herein defined; with a compound of formula (III) NH2OZ  (III) wherein Z is a hydroxy protecting group, in presence of a catalyst, to obtain a compound of formula (IV), or a salt thereof, removing the hydroxyl protecting group to obtain a compound of formula (V), or a salt thereof; converting a compound of formula (V), or a salt thereof, into a compound of formula (I), or a salt thereof; and, if desired, converting a compound of formula (I) into a salt thereof, or vice versa.

    摘要翻译： 制备式（I）化合物或其盐的方法，包括其中X和R如本文所定义的式（II）化合物的反应; 与式（III）化合物（其中Z为羟基保护基）在催化剂存在下反应，得到式（Ⅳ）化合物或其盐，除去羟基保护基，得到化合物 式（Ⅴ）化合物或其盐; 将式（Ⅴ）化合物或其盐转化为式（I）化合物或其盐; 如果需要，将式（I）化合物转化为其盐，反之亦然。

    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS
    8.
    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。