二丙酸倍他米松的合成研究

Synthesis of Betamethasone Dipropionate

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。

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.