Process for producing N-acylnitroaniline derivative
    25.
    发明授权
    Process for producing N-acylnitroaniline derivative 失效
    N-酰基硝基苯胺衍生物的制备方法

    公开(公告)号:US06630598B2

    公开(公告)日:2003-10-07

    申请号:US09903489

    申请日:2001-07-12

    申请人: Tomoyasu Yoshida

    发明人: Tomoyasu Yoshida

    IPC分类号: C07C20500

    摘要: A process of reacting a nitroaniline compound of formula (2): with an acid anhydride or acid halide is carried out in the presence of an alkali metal compound or an alkaline earth metal compound to produce an acylnitroaniline derivative. The process further includes the step of reacting the resulting product with a compound of formula (5); R2—Y to produce an N-acylnitroaniline derivative of formula (1): The N-acylnitroaniline derivative of formula (1) is a useful intermediate for the production of pharmaceuticals.

    摘要翻译: 使式(2)的硝基苯胺化合物与酸酐或酰卤反应的方法在碱金属化合物或碱土金属化合物的存在下进行,生成酰基硝基苯胺衍生物。 该方法还包括使所得产物与式(5)化合物反应的步骤;制备式(1)的N-酰基硝基苯胺衍生物:式(1)的N-酰基硝基苯胺衍生物是生产中的有用中间体 的药物。

    Perfluoroalkylated aniline compound and process for producing the same
    26.
    发明授权
    Perfluoroalkylated aniline compound and process for producing the same 有权
    全氟烷基化苯胺化合物及其制备方法

    公开(公告)号:US06600074B2

    公开(公告)日:2003-07-29

    申请号:US10206769

    申请日:2002-07-29

    IPC分类号: C07C21100

    摘要: The present invention provides an aniline derivative represented by the formula (I) wherein R1 and R2 are each H, (C1-12)alkyl, (C3-8)cycloalkyl, hydroxy(C1-12)alkyl, hydroxycarbonyl (C1-12)alkyl, (C1-6)-alkoxycarbonyl(C1-6)alkyl, —COR8, wherein R8 is H, halo-(C1-12)alkyl, (C3-8)cycloalkyl or (substituted) phenyl, COOR9, wherein R9 is a halo(C1-6)alkyl group, (substituted) phenyl or (substituted) benzyl; R3, R4, R5, R6and R7 are each H, halogen, OH, nitro, halo(C1-12)alkylthio, (substituted)amino-(C1-2)alkyl, (substituted) phenyl, (substituted) benzyl, amino, —N(R10)R11 wherein R10 and R11 are each H, alkyl, cycloalkyl, (substituted) phenyl, (substituted) benzyl, —COR8 or COOR9, or (C2-27)perfluoroalkyl, etc., and a process for producing the aniline derivative. According to the process of the present invention, perfluoroalkylaniline derivatives can be obtained by using various anilines as the substrate with a high position selectivity and high yield.

    摘要翻译: 本发明提供由式(I)表示的苯胺衍生物,其中R1和R2各自为H,(C1-12)烷基,(C3-8)环烷基,羟基(C1-12)烷基,羟基羰基(C1-12) 烷基,(C 1-6) - 烷氧基羰基(C 1-6)烷基,-COR 8,其中R 8为H,卤代(C 1-12)烷基,(C 3-8)环烷基或(取代)苯基,COOR 9,其中R 9为 (C 1-6)烷基,(取代的)苯基或(取代的)苄基; R3,R4,R5,R6和R7各自为H,卤素,OH,硝基,卤代(C1-12)烷硫基,(取代的)氨基 - (C1-2)烷基,(取代的)苯基,(取代的) -N(R 10)R 11其中R 10和R 11各自为H,烷基,环烷基,(取代)苯基,(取代的)苄基,-COR 8或COOR 9或(C 2- 27)全氟烷基等, 苯胺衍生物。 根据本发明的方法,可以通过以高位置选择性和高收率使用各种苯胺作为基材来获得全氟烷基苯胺衍生物。