| 引用本文: | 邓燕，何农跃，张永强，傅娟，张继德.喷昔洛韦的合成工艺研究[J].中国现代应用药学,2009,(9):737-739. |
| DENG Yan, HE Nongyue, ZHANG Yongqiang, FU Juan, ZHANG Jide.Improved Synthesis of Penciclovir[J].Chin J Mod Appl Pharm(中国现代应用药学),2009,(9):737-739. |
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| 摘要: |
| 目的以4-溴-2,2-二甲氧羰基-丁酸甲酯为原料合成新型抗病毒药物喷昔洛韦。方法采用2-氨基-6-氯嘌呤位置有择烷基化反应，缩合产物不经分离直接脱羧、还原、酰化、水解得到目标产物。结果总收率由文献的27%提高到33.1%。产物结构经元素分析、质谱、核磁共振氢谱及碳谱得到确证。结论该工艺简化了后处理操作，降低了原料成本，更易于工业化生产。 |
| 关键词: 喷昔洛韦 抗病毒药物 合成 |
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| Improved Synthesis of Penciclovir |
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DENG Yan, HE Nongyue, ZHANG Yongqiang, FU Juan, ZHANG Jide
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| Abstract: |
| OBJECTIVE To study the synthetic route of penciclovir, a kind of new antiviral drug, was synthesized with methyl 4-bromo-2, 2-bis-methoxycarbonyl-butyrate as raw material. METHODS Target compound was synthesized by means of the regioselective alkylation of 2-amino-6-chloropurine as a pivotal step, followed by decarboxylation, reduction, acetylation, and hydrolysis without separation of the products. RESULTS The total yield was amount to 33%, higher than literature. The target molecule was confirmed by MS, elementary analysis, 1H-NMR and 13C-NMR. CONCLUSION The improved process can be easily operated and is suitable for a scale production. |
| Key words: penciclovir antiviral drug synthesis |
