Hydrochloric Acid → HCID 9862994, compound

Participants

Reaction Steps

A solution of 1-[2-(N-ethylamino)-5-fluoro-4-(4-methyl-1-piperazinyl]phenyl-urea (640 mg) in methanol is treated with a freshly prepared methanolic solution of sodium methylate (from 150 mg of sodium) and heated under reflux for a short time. After cooling the solution is treated with diethyl malonate and stirred for 6 hours. The solution obtained is poured into a mixture of ice and 2N HCl (50 ml). The methanol is evaporated and the aqueous phase is extracted with ethyl acetate (3×100 ml) and methylene chloride (2×100 ml). After drying over magnesium sulfate the solvent mixture is evaporated and the residue is suspended in a small amount of cold ethyl acetate and filtered off. There are obtained 130 mg (17%) of 5-ethyl-8-fluoro-7-(4-methyl-1-piperazinyl)pyrimido[1,6-a]benzimidazole-1,3(2H,5H)-dione.

Provenance & Evidence