Herein we report, commercially available carbon-supported palladium (Pd/C) catalyzed N-methylation of nitroarenes and amines using MeOH as both C1 and H2 source. This transformation proceeds with high atom-economy and environmental-friendly way via borrowing hydrogen mechanism. A total of >30 structurally diverse N-methylamines, including bioactive compounds were selectively synthesized and isolated yields of up to 95%. Furthermore, selective N-methylation and deuteration of nimesulide, a nonsteroidal anti-inflammatory drug was realized through the late-stage functionalization.

Pd/C catalyzed N-methylation of nitroarenes and amines using MeOH offers a high atom-economy and environmentally friendly method for selective syntheses of bioactive compounds, including nimesulide.

Paper

Commercial Pd/C-Catalyzed N-Methylation of Nitroarenes and Amines using Methanol as Both C1 and H2 source.

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