PRODUCTION OF QUINAZOLINE-4-ONE DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To produce the subject quinazolinone that is powerful AMPA (- amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) acceptor antagonist and is useful for treatment of a variety of nervous disorders. SOLUTION: The objective compound, for example, 3-(chlorophenyl)-6- fluoro-2-[2-fluorophenyl]-2-hydroxyethyl]-3H-quinazoline-4-one}, is prepared by dehydration of 2-methylquinazoline derivative of formula I [R1 is a halogen, cyano, a 1-6C alkyl or the like; X is H, hydroxy, a halogen, trifluoromethyl, nitro or the like; Y is nitrogen or CH; Ar is a group of formula II (R2 is H or hydroxy; R4 and R7 are each H, a halogen, CF3 or the like)] with a dehydrating agent or by oxidizing the compound of formula I with an oxidizing agent.