Application and Progress of Organic Synthesis in the Discovery of Innovative Drugs

This article reviews the application and progress of modern synthetic methods to deliver several innovative drugs, especially the blockbusters, such as sofosbuvir, rivaroxaban, enzalutamide, canagliflozin and tofacitinib.Some of the modern synthetic methods, for example catalytic processes, application of ring-closing metathesis, palladium catalyzed cross-coupling, green chemistry and telescoping of processes, are highlighted.The exciting journey from discovering these new molecular entities, especially those which are first-in-class with the synthesis of a dozen of approved drugs, is described as case studies to fully illustrate the important role of modern organic synthesis for successful drug discovery and development.