摘要
目的:合成抗高血压药氯沙坦的关键中间体2-正丁基-4-氯-5-甲酰基咪唑。方法:戊腈与甲醇在甲醇钠的作用下加成得到1-甲氧基-1-亚胺戊烷(2),经取代、环合得到目标化合物2-正丁基-4-氯-5-甲酰基咪唑(1)。结论:本工艺具有试剂易得,反应条件温和,收率高(59.02%)的特点,适合工业化生产。
Objective：To synthesize a key intermediate of anti-hypertension drug Losartan,2-butyl-4-chloro-5-formylimidazole（1）.Methods：1-methoxy-1-imine pentane（2） was synthesized with methanol and valeronitrile as raw materials,catalyzed with sodium methoxide,and after substitution,by cyclization to obtain 2-butyl-4-chloro-5-formylimidazole（1）.Conclusion：This route was suitable for the large-scale preparation with its high yields（59.02%）,mild reaction conditions,easily available materials.
出处
《黑龙江医药科学》
2010年第4期18-19,共2页
Heilongjiang Medicine and Pharmacy
