发明公开
EP0015339A1 Separation of syn and anti 1-alkylsulfonyl-2-amino-5(6)hydroximinomethylbenzimidazole derivatives
失效
Trennung von syn-和抗-1-烷基磺酰基-2-氨基-5（6）肟基甲基苯并咪唑衍生物。
- 专利标题： Separation of syn and anti 1-alkylsulfonyl-2-amino-5(6)hydroximinomethylbenzimidazole derivatives
- 专利标题（中）： Trennung von syn-和抗-1-烷基磺酰基-2-氨基-5（6）肟基甲基苯并咪唑衍生物。
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申请号： EP79302272.4申请日： 1979-10-19
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公开(公告)号： EP0015339A1公开(公告)日： 1980-09-17
- 发明人: Shyan-Ell Su, Kenneth , Templeton, Robert Joseph , Wikel, James Howard
- 申请人： ELI LILLY AND COMPANY
- 申请人地址： 307, East McCarty Street Indianapolis Indiana 46285 US
- 专利权人： ELI LILLY AND COMPANY
- 当前专利权人： ELI LILLY AND COMPANY
- 当前专利权人地址： 307, East McCarty Street Indianapolis Indiana 46285 US
- 代理机构： Crowther, Terence Roger
- 优先权： US19526 19790312
- 主分类号： C07D235/30
- IPC分类号： C07D235/30
摘要：
To separate the syn and anti oximes of the formula
wherein R 1 is C 1 -C 5 alkyl; and R 2 is phenyl, or phenyl substituted by C 1 -C 4 alkyl, C 1 -C 4 alkoxy, chloro, bromo, iodo, nitro or trifluoromethyl, e.g. 1-isopropylsulfonyl-2-amino-6-(a-hydroximinobenzyl)-benzimidazole, a mixture of these oximes is dissolved in a water miscible organic solvent selected from methyl ethyl ketone, methanol, ethanol, isopropanol, acetonitrile, dimethylacetamide, dimethyl sulfoxide and, preferably, acetone, a sufficient quantity of water is added to initiate crystallization, and the precipitated anti oxime isomer which displays good antiviral activity is separated, e.g. in greater than about 95% purity.
wherein R 1 is C 1 -C 5 alkyl; and R 2 is phenyl, or phenyl substituted by C 1 -C 4 alkyl, C 1 -C 4 alkoxy, chloro, bromo, iodo, nitro or trifluoromethyl, e.g. 1-isopropylsulfonyl-2-amino-6-(a-hydroximinobenzyl)-benzimidazole, a mixture of these oximes is dissolved in a water miscible organic solvent selected from methyl ethyl ketone, methanol, ethanol, isopropanol, acetonitrile, dimethylacetamide, dimethyl sulfoxide and, preferably, acetone, a sufficient quantity of water is added to initiate crystallization, and the precipitated anti oxime isomer which displays good antiviral activity is separated, e.g. in greater than about 95% purity.
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