Abstract By listing the instances of medicinal chemistry teaching, this paper analyzed how to utilize the task-driven teaching mode to change the traditional way of medicinal chemistry teaching for the purpose of integrating inside and outside classroom teaching and cultivating students' learning initiatives. These examples included making cards of key drugs, carrying out small thematic teaching and writing book reports. Teaching practice indicated that making cards could both improve teaching efficiency and consolidate classroom teaching, small thematic teaching method could stimulate students' learning interests and cultivate their exploration spirits, and writing book reports could expand teaching contents.