3-Fluoro-4-(4-methyl-3-oxopiperazin-1-yl)nitrobenzene → 4-(4-Amino-2-fluorophenyl)-1-methylpiperazin-2-one

Participants

Reaction Conditions

Reaction Steps

3-Fluoro-4-(4-methyl-3-oxopiperazin-1-yl)nitrobenzene (3.33 g) was dissolved in a mixture of DMF (40 ml) and methanol (10 ml), and the solution flushed with argon. Ammonium formate (4.15 g) was added, and the mixture cooled to 5° C. Palladium (10% on carbon, 104 mg) was added, and the temperature allowed to rise to ambient as the mixture was stirred under argon for 2 hours. Solvents were evaporated to give an air sensitive product, 5-amino-2-(4-methyl-3-oxopiperazin-1-yl)fluorobenzene, which was used as such in the next stage.

Provenance & Evidence