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Medicinal chemistry is a very important subject in the pharmaceutical field, and it is also the necessary special knowledge and skill of the pharmacy job holders. Case-based learning (CBL) is an instructional design model that is a variant of project-oriented learning. It is the most appropriate teaching methodologies for training qualified pharmacy talents. Reasonable case–based learning can fully inspire the abilities and desires of the students' to analyze and solve problems. Students can broad their specialist knowledge, expand their field of vision during the process.