喷昔洛韦的合成工艺研究

• 作 者: 邓燕 何农跃 张永强 傅娟 张继德
• 机 构: 湖南工业大学绿色包装与生物纳米技术应用重点实验室,
• 出 处: 中国现代应用药学
• 发表日期: 2009年09期
• 关键词: 喷昔洛韦 抗病毒药物 合成

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。

OBJECTIVE To synthesize peniclovir, a novel antiviral drug, starting from 4-bromo-2,2-dimethoxycarbonyl-butyric acid methyl ester. Methods 2-amino-6-chloropurine position selective alkylation reaction, the condensation product directly without decarboxylation, reduction, acylation, hydrolysis of the target product. The total yield of results increased from 27% in the literature to 33.1%. The structure of the product was confirmed by elemental analysis, MS, 1H-NMR and GC-MS. Conclusion The process simplifies the post-processing operation, reducing the cost of raw materials, easier industrial production.