摘要
改进了碘海醇合成工艺中的关键步骤。在用醋酐酰化时用吡啶代替硫酸 ;在选择性水解时用氨水代替氢氧化钠 ;在 5 -位氮烷基化时用溶媒乙二醇单甲醚代替 1,2 -丙二醇。改进后的工艺反应条件温和、副反应少、易于操作 ,适于工业化生产 ,总收率 60 .8%。
Three key steps for the synthesis of iohexol were improved. Pyridine, ammonium hydroxide and 2 methoxyethanol were used instead of sulfuric acid, sodium hydroxide solution and propylene glycol in the steps of acylation, selective deacetylation and alkylation, respectively. The improved process is simpler, milder, less by products, and more suitable for scale up. The overall yield was 60.8%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2003年第6期261-262,共2页
Chinese Journal of Pharmaceuticals
关键词
碘海醇
造影剂
合成
iohexol
contrast agent
synthesis
