OBJECTIVE：To improve the synthesis technology of 7-methoxy-4-（2-methyl-4-quinazolinyl）-3，4-dihydroquinoxalin-2（1H）-ketone. METHODS： Using 2-methyl-4（3H）-quinazolone as starting material， the synthesis technology of 7-methoxy-4-（2-methyl-4-quinazolinyl）-3，4-dihydroquinoxalin-2（1H）-ketone was improved by clorination， nucleophilic substitution， diarylamine alkylation and nitro reductive cyclization. The yield of it was investigated. RESULTS： The structure of 7-methoxy-4-（2-methyl-4-quinazolinyl）-3，4-dihydroquinoxalin-2（1H）-ketone had been verified by 1H-NMR and ESI-MS. The yield was 43.5％ and improved by 23.3％ compared to 20.2％ before improvement. CONCLUSIONS： Improved technology is simpler and milder， which is suitable for the batch preparation of laboratory study.