药物化学综合性开放实验项目的构建——以“木香烃内酯衍生物的制备”为例

Construction of Medicinal Chemistry Comprehensive Open Experimental Project——The Case of“Preparation of Costunolide Derivative”

为了提高学生的实践能力、创新能力,合理利用实验室的资源,构建以药物化学为核心的药学综合性开放实验项目,作为传统实验教学的补充。以“木香烃内酯衍生物的制备”为例:从山玉兰根皮中提取分离得到木香烃内酯,筛选Brown硼氢化反应条件以48%的产率得到1位羟基衍生物2,并通过Mosher法确定了其绝对构型。确定该课题后,学生查阅文献,设计方案,再经教师审核和指导完成实验内容,最后形成实验总结和报告。该项目融合多个相关学科,有助于提高学生综合能力,实践中获得了学生较好的评价。

In order to improve students'practical ability and innovation ability,make full use of laboratory resources,a medicinal chemistry comprehensive open experimental project—“preparation of costunolide derivative”was constructed as a supplement to traditional experimental teaching:costunolide was extracted and isolated from Magnolia delavayi,Brown hydroboration reaction conditions were screened to obtain 1-hydroxy derivative 2 in 48%yield,and its absolute configuration was determined by Mosher method.After the subject is determined,students consult the literature,determine the experimental scheme,then complete experiment under the guidance of teacher,and finally form the experiment summary and report.The project integrates multiple related disciplines,which helps to improve students'comprehensive ability,and got a high evaluation by students in practice.