摘要
红霉素A硫氰酸盐与盐酸羟胺缩合成红霉素A-9-肟,红霉素肟与甲氧乙氧氯甲醚反应生成罗红霉素。研究了反应温度、反应时间以及物料配比对罗红霉素合成过程中杂质产生的影响,得到较优反应条件:n(红霉素肟):n(甲醇钠):n(甲氧基乙氧基氯甲醚)=1:1.12:1.21,甲醇钠和甲氧基乙氧基氯甲醚(MEMCl)的滴加时间分别为15min、45min;滴加甲醇钠时控制温度为5℃、滴加MEMCl的温度为0℃。此时的收率为95.8%(n/n)。
Reaction of thiocyanate erythromycin A with hydroxylamine hydrochloride afforded erythromycin A-9- oxime, followed by reaction with （methoxyethoxy） methyl chloride to form roxithromycin. Reaction conditions were optimized and the product was prepared in 95.8% yield. The reaction mechanism was proposed based on the analysis of by-products.
出处
《精细化工中间体》
CAS
2010年第2期44-47,共4页
Fine Chemical Intermediates
关键词
抗生素
罗红霉素
合成
antibiotic
roxithromyein
synthesis
impurity
