CHAPTER 15: Recent Large-Scale Applications of Transition Metal-Catalyzed Couplings for the Synthesis of Pharmaceuticals
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Published:13 Oct 2014
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Series: Catalysis Series
J. Magano and J. R. Dunetz, in New Trends in Cross-Coupling: Theory and Applications, ed. T. Colacot, The Royal Society of Chemistry, 2014, pp. 697-778.
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A review on recent applications of transition metal-catalyzed couplings on a large scale (>100 mmol) in the pharmaceutical industry is presented. Carbon–carbon, carbon–nitrogen and carbon–sulfur bond formation are discussed and relevant examples of each type of coupling are described with synthetic schemes that show the cross-coupling step and also the structure of the final active pharmaceutical ingredient (API). Special emphasis is placed on the practical aspects of these chemistries to make them amenable for scale-up. In addition, important issues such as metal removal to comply with stringent regulatory specifications are discussed.
