Hydrochloric Acid → Afloqualone

Participants

Reaction Steps

A mixture of 2.0 g of 2-fluoromethyl-3-(o-tolyl)-6-nitro-4(3H)-quinazolinone, 0.2 g of 5 % palladium-carbon and 100 ml of 10 % hydrochloric acid is shaken at 40°C for 1.5 hours in hydrogen gas. The initial pressure of hydrogen gas is adjusted to 48 lb. After said reaction, the mixture is cooled and filtered to remove the catalyst. The filtrate is neutralized with sodium bicarbonate, and the precipitate is extracted with benzene. The benzene solution is dried and then evaporated to remove solvent. The residue thus obtained is recrystallized from isopropanol. 1.3 g of 2-fluoromethyl-3-(o-tolyl)-6-amino-4(3H)-quinazolinone are obtained.

Provenance & Evidence