节点文献
氯替泼诺的合成工艺改进
Improved synthesis of loteprednol etabonate
【摘要】 以泼尼松龙为原料,经氧化、酰化、水解成盐、氯甲基化成酯制得氯替泼诺。用氯甲酸乙酯 将17位醇羟基和羧羟基同时酰化;水解时用碳酸钠溶液代替氢氧化钠甲醇溶液,提高反应的选择 性。改进后的工艺副反应少,操作简便,成本降低,总收率45%。
【Abstract】 Loteprednol etabonate was synthesized through oxidation, acylation, hydrolysis and chloromethy-lation from the starting material prednisolone. Ethyl chloroformate reacted with both the hydroxy group and’ the carboxy group of the 17 position. The sodium carbonate solution was used instead of sodium hydroxide’ s methanol solution in the step of selective hydrolysis. The modified technology is very convenient to operate with low consumption, and the overall yield is 45 % .
【关键词】 药物化学;
制备;
化学合成;
氯替泼诺;
【Key words】 medicinal chemistry; preparation; chemical synthesis; loteprednol etabonate;
【Key words】 medicinal chemistry; preparation; chemical synthesis; loteprednol etabonate;
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2003年05期
- 【分类号】TQ463
- 【被引频次】1
- 【下载频次】343