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ZHANG Chunlai, LUO Hongjun, JIANG Qi, LI Guoxian, GU Guoqing, ZHANG Jie. Improved process of dexrabeprazole sodium[J]. Journal of China Pharmaceutical University, 2018, 49(3): 291-294. DOI: 10.11665/j.issn.1000-5048.20180306
Citation: ZHANG Chunlai, LUO Hongjun, JIANG Qi, LI Guoxian, GU Guoqing, ZHANG Jie. Improved process of dexrabeprazole sodium[J]. Journal of China Pharmaceutical University, 2018, 49(3): 291-294. DOI: 10.11665/j.issn.1000-5048.20180306
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Improved process of dexrabeprazole sodium

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    • Abstract
  • The aim of the work is to improve the synthetic process of dexrabeprazole sodium, enhance quality and yield of the product, simplify synthetic steps, and offer a stable and feasible process. Starting from 2-［［［4-(3-methoxypropoxy)-3-methylpyridine-2-yl］methyl］ thio］-1H-benzimidazole, dexrabeprazole was produced by asymmetric oxidation reaction with oxidant cumene hydroperoxide in the presence of chiral catalyst tetraisopropyl titanate and L-(+)-tartaric acid diethyl ester. Dexrabeprazole sodium was obtained by the reaction of purified dexrabeprazole with sodium hydroxide in a total yield of 79% with an HPLC purity of > 99. 5%. The structure of dexrabeprazole sodium was confirmed by NMR, IR, elemental analysis and LC-MS. The improved process of dexrabeprazole sodium possesses simple operations, good yield and high purity, which is feasible for industrialization.
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    • References (19)
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