Micelle-Mediated Chemistry in Water for the Synthesis of Drug Candidates

Micellar reaction conditions, in a predominantly aqueous medium, have been developed for transformations commonly used by synthetic chemists working in the pharmaceutical industry to discover and develop drug candidates. The reactions covered in this review are the Suzuki-Miyaura, Miyaura borylation, Sonogashira coupling, transition-metal-catalysed C (Ar) -N coupling, S (N) Ar, amidation, and nitro reduction. Pharmaceutically relevant examples of these applications will be used to show how micellar conditions can offer advantages in yield, operational ease, amount of waste generated, transition-metal catalyst loading, and safety over the use of organic solvents, irrespective of the setting in which they are used. 1 Introduction 2 Micelles as Solubilising Agents 3 Micelles as Nanoreactors 4 Designer Surfactants 5 A Critical Evaluation of the Case for Chemistry in Micelles 6 Scope of Review 7 Suzuki-Miyaura Coupling 8 Miyaura Borylation 9 Sonogashira Coupling 10 Transition-Metal-Catalysed C (Ar) -N Couplings 11 S (N) Ar 12 Amidation 13 Nitro Reduction 14 Micellar Sequences 15 Summary and Outlook