A liquid-phase combinatorial synthesis of N-carbonylamido-2-(4-oxo-4H-1-benzopyran-3-yl)-4- thiazolidinones derivatives was successfully performed using N’-(chromon-3-yl)methylidene hydrazide de-rivatives and mercaptoacetic acid as reactants. Compared to an identical library generated by conventional parallel synthesis, the microwave-assisted parallel synthesis approach dramatically decreased the reaction time from an average of 8 h to 5 min, and substantially increased the product yields. The coupling of micro-wave technology with liquid-phase combinatorial synthesis constituted a novel and particularly attractive avenue for the rapid generation of structurally diverse libraries. At the same time, preliminary bioassay showed that part of them had insecticidal activities against Aphismedicagini at 250 μg•mL－1.

Key words: microwave-assisted combinatorial synthesis, chromone, insecticidal activity, thiazolidinone