The course is designed for undergraduate students that have passed successfully the medicinal chemistry I and II courses and have already completed a basic course in organic chemistry. The course will cover different methods to evaluate the structure of a target molecule through the retro-synthetic approach of that structure, and the strategies that can proceed for efficiently synthesizing that structure. The course will also cover the variety of tactics that can be employed for achieving the synthetic goal. At the completion of the course each student will demonstrate his/her mastery of these concepts by applying them to a complex and novel structure that has not yet succumbed to laboratory synthesis. Every student will randomly be given a different target molecule, with each structure presenting its own unique challenges. The student will derive a strategy for the synthesis of the target molecule and will then outline and justify a plan for its synthesis from readily-available starting materials using all available tactics.