4-(2,6-Difluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester → 4-(4-Amino-2,6-difluorophenyl)piperazine, N1-BOC protected

Beteiligte Stoffe

Reaktionsschritte

To a solution of 4-(2,6-difluoro-4-nitro-phenyl)-piperazine-1-carboxylic acid tert-butyl ester (Intermediate II) (30 g, 0.09 mol), in methanol (500 mL) under argon atmosphere was added 10% Pd/C (4.5 g, 15 mol% by weight). Flask was evacuated and hydrogen was introduced with the help of balloon. The reaction mixture was stirred under hydrogen and progress of the reaction was monitored by TLC. On completion, the reaction mixture was filtered through celite pad using methanol as solvent. The filterate was evaporated to provide title compound (26 g, 95%) as pale yellow solid.

Herkunft & Nachweise