二丙酸倍他米松的合成研究

Synthesis of Betamethasone Dipropionate

摘要: 目的合成二丙酸倍他米松。方法以倍他米松为原料，经过酸催化17，21-环合、选择性水解和21位丙酰化3步反应，合成倍他米松-17，21-双丙酸酯。结果目标物经IR、¹H-NMR、¹³C-NMR和MS确证结构，反应总收率达到76.4%，HPLC纯度为99.56%。结论该合成路线操作简便、反应条件温和，适于工业化生产。

Abstract: OBJECTIVE Synthesis of betamethasone dipropionate. METHODS The betamethasone dipropionate was synthesized from betamethasone through acid catalysis cyclization, selective hydrolysis and 21-acylation. RESULTS The structure of product was identified by IR, ¹H-NMR, ¹³C-NMR and MS, the total yield was 76.4% and the HPLC purity was 99.56%. CONCLUSION The synthetic process is simple, easy to control and suitable for industrial production.