Palladium‐Catalyzed Methylation of Nitroarenes with Methanol

A procedure for the synthesis of N‐methyl‐arylamines directly from nitroarenes using methanol as green methylating agent was developed. Key to success is the use of a specific catalyst system consisting of palladium acetate and the ligand 1‐​[2,​6‐​bis(isopropyl)​phenyl]​‐​2‐​[tert‐butyl(2‐pyridinyl)phosphi​no]​‐1H‐​Imidazole (L1). The generality of this protocol is demonstrated in the synthesis of more than 20 N‐methyl‐arylamines under comparably mild conditions. Combining this novel methodology with subsequent coupling processes using the same catalyst allows for efficient diversification of aromatic nitro compounds to a broad variety of amines including drug molecules.

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