This article describes three historical cases of drug discovery and how they were adapted as examples to teach chemical analysis to students pursuing a pharmacy (UK MPharm) and pharmaceutical sciences (BSc Pharmaceutical Sciences) degree. The selected cases were the synthesis of benzodiazepines and the discovery of warfarin and neuromuscular blocking agents. These examples present some peculiarities as they were developed in special circumstances and without the assistance of modern chemical analysis techniques. By incorporating these examples in a pharmaceutical chemistry class, the students became aware of the importance of chemical knowledge in overcoming technical limitations. Moreover, the examples were designed to stimulate the interest of the students in the subject. Three case studies including drug discovery examples were implemented in a chemistry module delivered to pharmacy students. The views of the students (48 MPharm and 7 BSc pharmaceutical sciences) about these lectures was obtained by using a questionnaire. After delivering the lectures, the majority of the students (64%) thought that understanding the history behind some scientific discoveries was important for them. Additionally, they considered that the selected historical examples were not only interesting but useful to understand the material delivered in the pharmaceutical chemistry module (75% of the students).