- 专利标题: Method for producing aminothiazole derivative and production intermediate
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申请号: EP10010897.6申请日: 2005-08-23
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公开(公告)号: EP2269975A3公开(公告)日: 2011-02-16
- 发明人: Nagasawa, Masaaki , Asami, Kazuyasu , Nakao, Ryu , Tanaka, Nobujuki , Aida, Yoshiyuki
- 申请人: ZERIA PHARMACEUTICAL CO., LTD.
- 申请人地址: 10-11, Nihonbashi Kobuna-cho, Chuo-ku Tokyo 103-8351 JP
- 专利权人: ZERIA PHARMACEUTICAL CO., LTD.
- 当前专利权人: ZERIA PHARMACEUTICAL CO., LTD.
- 当前专利权人地址: 10-11, Nihonbashi Kobuna-cho, Chuo-ku Tokyo 103-8351 JP
- 代理机构: Blodig, Wolfgang
- 优先权: JP2004242759 20040823
- 主分类号: C07C67/08
- IPC分类号: C07C67/08 ; C07C67/11 ; C07C69/92 ; C07D277/20 ; C07D277/56 ; C07C51/377
摘要:
A production method of a compound represented by formula (2):
(wherein ring A represents a benzene ring or a 6-membered aromatic heterocycle; R 1 represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a nitro group, an amino group, a mono-C 1-6 alkylamino group, or a di-C 1-6 alkylamino group; and at least one of R 2 , R 3 , and R 4 represents a methoxy group, and the rest each represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a nitro group, an amino group, a mono-C 1-6 alkylamino group, or a di-C 1-6 alkylamino group),
comprising reacting a compound represented by formula (1):
(wherein ring A and R 1 , R 2 , R 3 , and R 4 are the same as defined above) with a Lewis acid selected from BF 3 , TiCl 4 , and AlCl 3 in esteric, ketonic or amidic solvents selected from ethyl acetate, methyl acetate, butyl acetate, isobutyl acetate, acetone, 2-butane, cyclohexane, cyclopentane, dimethylformamide, and dimethylacetamide, with the proviso that when the Lewis acid is BF 3 , an alkali metal bromide or an alkali metal iodide coexists.
(wherein ring A represents a benzene ring or a 6-membered aromatic heterocycle; R 1 represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a nitro group, an amino group, a mono-C 1-6 alkylamino group, or a di-C 1-6 alkylamino group; and at least one of R 2 , R 3 , and R 4 represents a methoxy group, and the rest each represents a hydrogen atom, a C 1-6 alkyl group, a halogen atom, a nitro group, an amino group, a mono-C 1-6 alkylamino group, or a di-C 1-6 alkylamino group),
comprising reacting a compound represented by formula (1):
(wherein ring A and R 1 , R 2 , R 3 , and R 4 are the same as defined above) with a Lewis acid selected from BF 3 , TiCl 4 , and AlCl 3 in esteric, ketonic or amidic solvents selected from ethyl acetate, methyl acetate, butyl acetate, isobutyl acetate, acetone, 2-butane, cyclohexane, cyclopentane, dimethylformamide, and dimethylacetamide, with the proviso that when the Lewis acid is BF 3 , an alkali metal bromide or an alkali metal iodide coexists.
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