丙酸氟替卡松的合成
Synthesis of Fluticasone propionate
作者:刘金仙;马晓莉;马丽芳;李子元;
Author:
收稿日期: 年卷(期)页码:2007,(01):-51-53
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:丙酸氟替卡松;糖皮质激素;合成
Key words:
基金项目:
中文摘要
目的合成丙酸氟替卡松。方法以氟米松(2)作为起始原料,经高碘酸氧化、丙酰化得到4;4与N,N-二甲基硫代氨基甲酰氯反应生成5;5与BrCH2Cl在K2CO3存在的条件下反应生成6;6与KF在丙酮中回流生成1。结果五步反应总收率为47.8%,产物经MS1、HNMR确证结构。结论改进后的方法避免使用对臭氧层有害且价昂的BrCH2F,收率相当。
参考文献
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