| 引用本文: | 张宇松,金炜华,汪卫军.二丙酸倍他米松的合成研究[J].中国现代应用药学,2011,28(7):648-650. |
| ZHANG Yusong,JIN Weihua,WANG Weijun.Synthesis of Betamethasone Dipropionate[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(7):648-650. |
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| 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。 |
| 关键词: 二丙酸倍他米松 前药 糖皮质激素 合成 |
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| Synthesis of Betamethasone Dipropionate |
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ZHANG Yusong, JIN Weihua, WANG Weijun
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Zhejiang Xianju Pharma Ltd., Xianju, 317300, China
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| 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. |
| Key words: betamethasone dipropionate prodrug glucocorticoid synthesis |
