transition metal catalyzed couplings in process chemistry case studies from the pharmaceutical industry

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Transition Metal Catalyzed Couplings In Process Chemistry

Author : Javier Magano
ISBN : 9783527658923
Genre : Science
File Size : 47. 77 MB
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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.

Handbook For Chemical Process Research And Development

Author : Wenyi Zhao
ISBN : 9781315350202
Genre : Medical
File Size : 69. 54 MB
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The Handbook for Chemical Process Research and Development focuses on developing processes for chemical and pharmaceutical industries. Forty years ago there were few process research and development activities in the pharmaceutical industry, partially due to the simplicity of the drug molecules. However, with the increasing structural complexity, especially the introduction of chiral centers into the drug molecules and strict regulations set by the EMA and FDA, process R&D has become one of the critical departments for pharmaceutical companies. This book assists with the key responsibility of process chemists to develop chemical processes for manufacturing pharmaceutical intermediates and final drug substances for clinical studies and commercial production.


Author : Meng Li
ISBN : 9781849736749
Genre :
File Size : 36. 34 MB
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This book is an essential resource for anyone interested in the chemistry and applications of boron.

Synthetic Methods In Drug Discovery

Author : David C. Blakemore
ISBN : 9781849738033
Genre :
File Size : 60. 48 MB
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The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.

Catalytic Arylation Methods

Author : Anthony J. Burke
ISBN : 9783527672851
Genre : Science
File Size : 27. 30 MB
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This "hands-on" approach to the topic of arylation consolidates the body of key research over the last ten years (and up to around 2014) on various catalytic methods which involve an arylation process. Clearly structured, the chapters in this one-stop resource are arranged according to the reaction type, and focus on novel, efficient and sustainable processes, rather than the well-known and established cross-coupling methods. The entire contents are written by two authors with academic and industrial expertise to ensure consistent coverage of the latest developments in the field, as well as industrial applications, such as C-H activation, iron and gold-catalyzed coupling reactions, cycloadditions or novel methodologies using arylboron reagents. A cross-section of relevant tried-and-tested experimental protocols is included at the end of each chapter for putting into immediate practice, along with patent literature. Due to its emphasis on efficient, "green" methods and industrial applications of the products concerned, this interdisciplinary text will be essential reading for synthetic chemists in both academia and industry, especially in medicinal and process chemistry.

Catalytic Process Development For Renewable Materials

Author : Pieter Imhof
ISBN : 9783527656653
Genre : Science
File Size : 25. 74 MB
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Green, clean and renewable are the hottest keywords for catalysis and industry. This handbook and ready reference is the first to combine the fields of advanced experimentation and catalytic process development for biobased materials in industry. It describes the entire workflow from idea, approach, research, and process development, right up to commercialization. A large part of the book is devoted to the use of advanced technologies and methodologies like high throughput experimentation, as well as reactor and process design models, with a wide selection of real-life examples included at each stage. The contributions are from authors at leading companies and institutes, providing firsthand information and knowledge that is hard to find elsewhere. This work is aimed at decision makers, engineers and chemists in industry, chemists and engineers working with/on renewables, chemists in the field of catalysis, and chemical engineers.

Organometallics As Catalysts In The Fine Chemical Industry

Author : Matthias Beller
ISBN : 3642442587
Genre : Science
File Size : 80. 62 MB
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Johannes G. de Vries: Pd-catalyzed coupling reactions.- Gregory T. Whiteker and Christopher J. Cobley: Applications of Rhodium-Catalyzed Hydroformylation in the Pharmaceutical, Agrochemical and Fragrance Industries.- Philippe Dupau: Ruthenium-catalyzed Selective Hydrogenation for Flavor and Fragrance Applications.- Hans-Ulrich Blaser, BenoƮt Pugin and Felix Spindler: Asymmetric Hydrogenation.- Ioannis Houpis: Case Study: Sequential Pd-catalyzed Cross-Coupling Reactions; Challenges on Scale-up.- Adriano F. Indolese: Pilot Plant Scale Synthesis of an Aryl-Indole - Scale up of a Suzuki Coupling.- Per Ryberg: Development of a Mild and Robust Method for Palladium Catalysed Cyanation on Large Scale.- Cheng-yi Chen: Application of Ring Closing Metathesis Strategy to the Synthesis of Vaniprevir (MK-7009), a 20-Membered Macrocyclic HCV Protease Inhibitor.

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