A simple and efficient method was developed for the synthesis of 2,6-dimethyl-3-aryl-4(1H)-quinolones via the acylation and cyclization of N-(4-methylphenyl)acetamide with substituted phenylacetic acids under microwave irradiation. The reaction conditions of acylation and cyclization were optimized, and the reaction time was shortened enough. N-(4-Methyl-2-(2-arylacetyl)phenyl)acetamides were synthesized with 85.7%～91.3% yields by the acylation of N-(4-methylphenyl)acetamide and substituted phenylacetic acids using BF3?Et2O as catalyst under the conditions of microwave irradiation, 80 ℃ and 15 min. In the presence of sodium tert-butanolate and tert-butanol, the cyclization of N-(4-methyl-2-(2-arylacetyl)phenyl)acetamides under microwave irradiation and reflux condition were completed within 20 min giving the target compounds 2,6-dimethyl-3-aryl-4(1H)-quinolones in 89.2%～94.3% yields. The structures of the target compounds were identified by IR, 1H NMR spectra and elemental analysis.