Transition metal-catalyzed coupling reactions have a significant history, culminating in the 2010 Nobel Prize in Chemistry awarded to Professors Suzuki, Heck, and Negishi for their groundbreaking work. This book highlights the maturation of this research area through case studies where process chemists from the pharmaceutical industry recount their experiences in developing transition metal-catalyzed couplings for the large-scale production of active pharmaceutical ingredients. Contributors from Pfizer, Merck, Boehringer-Ingelheim, Novartis, Amgen, GSK, AstraZeneca, and others detail the progression of robust coupling processes from initial conception to commercial routes, when applicable. A broad spectrum of coupling transformations is explored, emphasizing the lessons learned throughout each process. Each case study focuses on the optimization of at least one transition metal-catalyzed coupling, addressing critical aspects such as experimental design, scalability, product purification, process safety, and waste management. The book also tackles the vital issue of metal removal and the various technologies available for this purpose. Additionally, it presents innovative technologies for cross-coupling with significant future potential, including microwave and flow chemistry, as well as environmentally friendly cross-couplings conducted in water. Forewords are provided by notable figures in the field.
