Abstract: Three novel 2-((4, 4-dimethyl-3-oxoisoxazolidin-2-yl)methyl)-3-aryl acrylate derivatives were designed and synthesized utilizing Baylis-Hillman adducts as starting materials, based on the Clomazone (FMC-57020) [2-(2-chlorobenzyl)-4, 4-dimethylisoxazolidin-3-one] which is a low-toxicity high-efficiency soybean herbicide developed by FMC Corporation in the USA. The structures of the compounds were confirmed by IR, 1H NMR and elemental analysis. An evaluation done for their biological activities indicated that the target compounds 3 exhibit efficiently the herbicidal activity at 2000 g ai/hm², while the intermediate ethyl 2-(bromomethyl)-3-(2, 4-dichloro phenyl) acrylate (2 b) shows insecticidal activity with a thorough control of tetranychus cinnabarinus at 600 g ai/hm². Because of the herbicidal activities found in all the acrylate derivatives (3), they may be regarded as the lead herbicidal compounds to study further.