Applications of Transition Metal Catalysis in Drug Discovery and Development: An Industrial Perspective
This book focuses on the drug discovery and development applications of transition metal catalyzed processes, which can efficiently create preclinical and clinical drug candidates as well as marketed drugs. The authors pay particular attention to the challenges of transitioning academically-developed reactions into scalable industrial processes. Additionally, the book lays the groundwork for how continued development of transition metal catalyzed processes can deliver new drug candidates. This work provides a unique perspective on the applications of transition metal catalysis in drug discovery and development – it is a guide, a historical prospective, a practical compendium, and a source of future direction for the field.
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Selected Applications of Transition MetalCatalyzed
Selected Applications of Pd and CuCatalyzed CarbonHeteroatom
Asymmetric CrossCoupling Reactions
Transition MetalCatalyzed Synthesis of Five and SixMembered
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active alcohol alkylation allylic amination Angew applications aryl aryl bromide asymmetric hydrogenation asymmetric synthesis biaryl BINAP Bioorg BocHN boronic acid Buchwald C–C bond C–N coupling catalyst catalyst loading catalyst system Chem chemical chemistry chemists chiral chloride Cl Cl CO2H CO2Me complex compound coupling reactions coworkers cross-coupling reactions Cu-catalyzed cyclization developed diastereoselective double bond drug discovery efficient enantiomeric excess enantioselective epoxidation equiv ester example formation Hartwig Heck coupling Heck reaction inhibitor intermediate ketone large-scale ligand macrocyclic Merck metathesis molecules Negishi coupling nucleophile olefin optimization oxidation Pd-catalyzed Pfizer pharmaceutical industry PPh2 Process Res reagents receptor antagonist reflux route scale Sharpless Shibasaki shown in Scheme solvent Sonogashira coupling steps substrate Suzuki coupling synthetic Tetrahedron Lett toluene transition metal transition metal-catalyzed triflate Trost Wang Zhang