药物合成前沿技术融入药学专业本科生综合化学实验教学的探索与实践——盐酸苯海索的制备与精制

Exploring and Practice of Integrating Frontier Medicine Synthetic Technology into Comprehensive Chemical Experiment for Undergraduates Majoring in Pharmacy:Preparation and Purification of Benzoxol Hydrochloride

设计了一种合成中枢抗胆碱抗帕金森病药物盐酸苯海索的反应路线,并通过教学实践指导本科生独立自主的通过曼尼希反应、格氏反应制备关键中间体,进一步合成纯度达到95%以上的盐酸苯海索。本实验可以锻炼学生的药物合成能力,熟悉小分子药物的一般制备方法及其性质检测方法,并能很好的掌握化学合成仪器设备的使用,由特定药物合成扩展到一般性、普适性,使学生进一步了解药学尤其是药物化学科学前沿,提升学生的科学素养。

A reaction route for synthesis of central anti-choline and anti-Parkinson's drug benhyxol hydrochloride was designed,and through teaching practice,undergraduates were instructed to independently prepare key intermediates through Mannich reaction and Grainger reaction,and further synthesis of benhyxol hydrochloride with purity of more than 95%.This experiment can exercise students'ability of drug synthesis,get familiar with the general preparation methods and properties detection methods of small molecule drugs,and master the use of chemical synthesis instruments and equipment well,from specific drug synthesis to general,universal,so that students can further understand pharmacy,especially pharmaceutical chemistry science frontier,improve students'scientific literacy.