发明公开
EP2486032A2 OPTICAL RESOLUTION OF SUBSTITUTED 2-(2- PYRIDINYLMETHYLSULPHINYL)-1H-BENZIMIDAZOLES
审中-公开
分辨率取代的2-(2-吡啶基甲基)-1H-苯并咪唑
- 专利标题: OPTICAL RESOLUTION OF SUBSTITUTED 2-(2- PYRIDINYLMETHYLSULPHINYL)-1H-BENZIMIDAZOLES
- 专利标题(中): 分辨率取代的2-(2-吡啶基甲基)-1H-苯并咪唑
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申请号: EP09850200.8申请日: 2009-10-09
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公开(公告)号: EP2486032A2公开(公告)日: 2012-08-15
- 发明人: PARTHASARADHI REDDY, Bandi , RATHNAKAR REDDY, Kura , RAJI REDDY, Rapolu , MURALIDHARA REDDY, Dasari , VAMSI KRISHNA, Bandi , SATYA SRINIVAS, Ayyalasomayajula
- 申请人: Hetero Research Foundation
- 申请人地址: Plot No. B-80&81 A.P.I.E., Balanagar Hyderabad 500 018, Andhrapradesh IN
- 专利权人: Hetero Research Foundation
- 当前专利权人: Hetero Research Foundation
- 当前专利权人地址: Plot No. B-80&81 A.P.I.E., Balanagar Hyderabad 500 018, Andhrapradesh IN
- 代理机构: Thomas, Simon
- 国际公布: WO2011042910 20110414
- 主分类号: C07D401/12
- IPC分类号: C07D401/12
摘要:
The present invention relates to process for preparation of optical resolution of substituted 2-(2-pyridinylmethylsulphinyl)-1H-benzimidazoles either as a single enantiomer or in an enantiomerically enriched form. Thus, for example, R-1,1'-binaphtyl- 2-2'-diyl hydrogen phosphate was reacted with 2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)- 2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole (Lansoprazole) in a mixture of benzene and cyclohexane to obtain diasteremeric complexes. The diasteremeric complexes were subjected to fractional crystallization to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro- ethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole.R-1,1'-binaphthyl-2-2'-diyl hydrogen phosphate. The separated isomer was treated with sodium bicarbonate in a mixture of ethyl acetate and water to obtain R-2-[[[3-methyl-4-(2,2,2-trifluoro-ethoxy)-2- pyridinyl]methyl]sulfinyl]-1H-benzimidazole (dexlansoprazole).
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