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Transition Metal-Catalyzed Couplings in Process Chemistry Case Studies from the Pharmaceutical Industry (Hardcover)
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Transition Metal-Catalyzed Couplings in Process Chemistry Case Studies from the Pharmaceutical Industry (Hardcover)
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Transition metal-catalyzed coupling reactions have a rich history
that led to the awarding of the 2010 Nobel Prize in Chemistry to
Professors Suzuki, Heck, and Negishi for their pioneering
contributions to the field. The coming of age of this active area
of research is showcased in this book through case studies in which
process chemists from the pharmaceutical industry share their
personal experiences developing their own transition
metal-catalyzed couplings for the large-scale manufacture of active
pharmaceutical ingredients. Authors from Pfizer, Merck,
Boehringer-Ingelheim, Novartis, Amgen, GSK, AstraZeneca, and other
companies describe the evolution of robust coupling processes from
inception through early and late development, including commercial
routes where applicable. This book covers a wide range of coupling
transformations while capturing the lessons learned from each
process. Every case study details the optimization of at least one
transition metal-catalyzed coupling while elaborating on issues
such as design of experiments, scalability and throughput, product
purification, process safety, and waste management. The important
issue of metal removal and the different technologies available to
accomplish this goal are also addressed. Finally, a section covers
novel technologies for cross-coupling with high potential for
future applications on a large scale, such as microwave and flow
chemistry as well as green cross-couplings performed in water. With
Forewords by Stephen L. Buchwald, Massachusetts Institute of
Technology, Trevor Laird, Editor of Organic Process Research and
Development and Neal G. Anderson, Anderson's Process Solutions LLC.
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