公开(公告)号：EP1798216A1

公开(公告)日：2007-06-20

申请号：EP05785694.0

申请日：2005-09-26

申请人： Sankyo Company, Limited

发明人： KAJINO, Hisaki c/o Sankyo Company Limited ,  MIYAMOTO, Hiroshi c/o Sankyo Company Limited ,  IKEUCHI, Yutaka c/o Sankyo Company Limited

IPC分类号： C07C217/84 ,  C07C211/52 ,  C07C209/10 ,  C07C213/00 ,  C07C271/28 ,  C07D277/20 ,  C07D277/34 ,  C07D417/12

CPC分类号： C07D277/34 ,  C07C217/90 ,  C07C271/28 ,  C07C323/36 ,  C07D417/12

摘要： [Subject]
The object of the present invention is to provide new intermediates (IIa) and (III) of the 6-substituted-1-methyl-1-H-benzimidazol derivatives (I) which are publicly known pharmaceutically active ingredients, and a preparation procedure suitable for a large scale synthesis of N-(5-substituted-2-nitrophenyl)-N-methylamines (II) which are synthetic intermediates.
Additionally, another object of the present invention is to provide an efficient procedure for the preparation of the 6-substituted-1-methyl-1-H-benzimidazole derivative (I) from said synthetic intermediates (II) in a shorter number of steps.
[Measures to solve the subject]
The present invention relates to a procedure for the preparation of a compound (I) represented by the following formula and synthetic intermediates of said compound (I).

(In the above reaction scheme, R 2 represents a phenyl group which may optionally be substituted with substituents such as a C 1 -C 6 alkyl group or the like, and X represents an oxygen atom, a sulfur atom or a nitrogen atom).

摘要翻译： [主题]本发明的目的是提供一种高级的中间体（IIa）和（III）的6- substituiertem -1-甲基-1H-苯并咪唑衍生物（I），其是公知的药学活性成分，和一个的 适合的N-大规模合成制备程序（5-取代的-2-硝基苯基）-N-甲基胺（II），其是合成的中间体。 另外，本发明的另一目的是提供高效程序为6- substituiertem -1-甲基-1H-苯并咪唑从在更短的多个步骤，所述合成中间体（II）衍生物（Ⅰ）的制备方法。 [处理方法来解决所述对象本发明涉及一种用于由下式和所述化合物（I）的合成中间体表示的化合物（I）的制备过程。 （在上述反应路线中，R 2表示可以任选被检查为C 1 -C 6烷基或类似物，且X darstellt到氧原子，硫原子或氮原子的取代基substituiertem苯基）。