To provide a production method of a new synthetic method of febrifugine (3-[3-(3-hydroxy-2-piperidinyl)-2-oxopropyl]-4(3H)-quinazolinone) and isofebrifugine having very strong activity against tropical malaria parasite by total synthesis route of carrying out the whole steps in an aqueous solvent.

A protector of the objective material is prepared by using (R)-(+)-2,2-dimethyl-1,3-dioxolane-4-carboxaldehyde as a starting material, subjecting the material to several steps to afford (3'S)-1-[2'-(3'-benzyloxy)-1'-(tert-butoxycarbonyl)-piperidino]-3-hydroxy-2-propanone, and reacting the product with 4-hydroxyquinazoline. The febrifugine is prepared by subjecting the protector to heat treatment with 6N hydrochloric acid.