发明公开
EP1798216A1 INTERMEDIATE OF 6-SUBSTITUTED-1-METHYL-1-H-BENZIMIDAZOLE DERIVATIVE AND METHOD FOR PRODUCING SAME
审中-公开
6-取代的1-甲基-1H-苯并咪唑衍生物的中间体及其制造方法
- 专利标题： INTERMEDIATE OF 6-SUBSTITUTED-1-METHYL-1-H-BENZIMIDAZOLE DERIVATIVE AND METHOD FOR PRODUCING SAME
- 专利标题（中）： 6-取代的1-甲基-1H-苯并咪唑衍生物的中间体及其制造方法
-
申请号： EP05785694.0申请日： 2005-09-26
-
公开(公告)号： EP1798216A1公开(公告)日： 2007-06-20
- 发明人: KAJINO, Hisaki c/o Sankyo Company Limited , MIYAMOTO, Hiroshi c/o Sankyo Company Limited , IKEUCHI, Yutaka c/o Sankyo Company Limited
- 申请人： Sankyo Company, Limited
- 申请人地址： 5-1, Nihonbashi Honcho 3-chome, Chuo-ku Tokyo 103-8426 JP
- 专利权人： Sankyo Company, Limited
- 当前专利权人： Sankyo Company, Limited
- 当前专利权人地址： 5-1, Nihonbashi Honcho 3-chome, Chuo-ku Tokyo 103-8426 JP
- 代理机构： Andrews, Timothy Stephen
- 优先权： JP2004282064 20040928
- 国际公布： WO2006035685 20060406
- 主分类号： C07C217/84
- IPC分类号： C07C217/84 ; C07C211/52 ; C07C209/10 ; C07C213/00 ; C07C271/28 ; C07D277/20 ; C07D277/34 ; 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).
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).
信息查询
