公开(公告)号：US06624179B1

公开(公告)日：2003-09-23

申请号：US10030122

申请日：2002-01-24

申请人： Toru Koyanagi ,  Yuji Nakamura ,  Masayuki Morita ,  Tsuyoshi Ueda ,  Akihiro Hisamatsu ,  Mayumi Kanamori

发明人： Toru Koyanagi ,  Yuji Nakamura ,  Masayuki Morita ,  Tsuyoshi Ueda ,  Akihiro Hisamatsu ,  Mayumi Kanamori

IPC分类号： A61K3144

CPC分类号： C07C329/16 ,  C07B2200/09 ,  C07C255/34 ,  C07C255/38 ,  C07C329/04 ,  C07C329/06

摘要： A geometrical isomer of an acrylonitrile compound represented by the formula (I) or of its salt, or a mixture thereof: [wherein T is phenyl or pyridyl, which is substituted by R2, Q is phenyl, thienyl, pyridyl or benzyl, which may be substituted by R3, R1 is —C(═O)R4 or —C(═S)R4, R4 is alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, cycloalkyl, cycloalkyloxy, cycloalkylthio, —N(R5)R6, phenyl, phenoxy, phenylthio, benzyl, benzyloxy, benzylthio, —J, —O—J or —S—J], wherein the geometrical isomer has a longer retention time when analyzed by reversed phase liquid chromatography in which a packing comprising silica having chemically bonded thereto an alkyl group selected from trimethyl, octyl and octadecyl, is used as the stationary phase, and a polar solvent selected from water, methanol and acetonitrile, is used as the mobile phase, and the geometrical isomer mixture contains such geometrical isomer in a larger proportion.

摘要翻译： 由式（I）表示的丙烯腈化合物或其盐的几何异构体或其混合物：[其中T是被R 2取代的苯基或吡啶基，Q是苯基，噻吩基，吡啶基或苄基，其可以 被R 3取代，R 1是-C（= O）R 4或-C（= S）R 4，R 4是烷基，烯基，炔基，烷氧基，烯氧基，炔氧基，烷硫基，链烯硫基，炔硫基，环烷基，环烷氧基， N（R 5）R 6，苯基，苯氧基，苯硫基，苄基，苄氧基，苄硫基，-J，-OJ或-SJ]，其中几何异构体在通过反相液相色谱分析时具有更长的保留时间， 化学键合有选自三甲基，辛基和十八烷基的烷基作为固定相，使用选自水，甲醇和乙腈的极性溶剂作为流动相，几何异构体混合物含有这种几何异构体 比例较大。