The development of palladium‐catalyzed α‐arylation of carbonyl compounds has emerged as a new avenue in the design of new routes for the synthesis of natural products and active pharmaceutical ingredients (APIs). In many cases, syntheses based on α‐arylation strategies provide elegant routes in terms of increasing the overall yields, improving the synthesis scope, and decreasing the number of steps. This microreview aims to highlight the importance of palladium‐catalyzed α‐arylation methodologies, covering a range of notable reported examples of the total syntheses of structurally important compounds, thereby highlighting the importance of this powerful methodology for key steps in organic synthesis.
The cover picture shows the scope of the α‐arylation reaction of carbonyl compounds, such as ketones, aldehydes, esters and amides in the total syntheses of natural products and active pharmaceutical ingredients (API). This is exciting, because α‐arylation reactions have emerged recently as one of the new trends in cross‐coupling reactions, in which the CH at the α position of the carbonyl group undergoes functionalization by enolization in the presence of a base, followed by a C–C coupling under the influence of a metal catalyst, typically Pd. The potential of this powerful methodology will be enormous for key steps in organic synthesis for small and large molecules. Details are presented in the Microreview by T. J. Colacot et al. on .
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