2-巯基-5-甲氧基苯并咪唑合成工艺的研究

Study on Synthesis of 2-Mercapto-5-Methoxybenzimidazole

关键词:  奥美拉唑  2-巯基-5-甲氧基苯并咪唑  雷尼镍  催化加氢  醋酸硝酰

Key words:  Omeprazole  2-Mercapto-5-Methoxybenzimidazole  Ranney nickel  catalytic hydrogenation  nitroxyl acetate

摘要:

目的改进2-巯基-5-甲氧基苯并咪唑的合成工艺。方法以对氨基苯甲醚为起始原料,采用醋酸硝酰作硝化剂进行硝化;采用雷尼镍催化加氢法进行还原。结果制得了奥美拉唑中间体2-巯基-5-甲氧基苯并咪唑,总收率78.5%。结论值得推广到工业化生产。

Abstract:

OBJECTIVE To improve the synthetic process of 2-Mercapto-5-Methoxybenzimidazole(1).METHODS Product(1) was synthesized from p-aminoanisole by acetylation,nitrification,hydrolysis,reduction and cyclic condensation.The nitrifying agent was nitroxyl acetate,a