Abstract: Etoxazole, discovered by Yashima Chemical Industry Co. Ltd. and launched in 1998, is the only commercialized acaricide of 2,4-diphenyl-1,3-oxazolines. It has unique mechanism of inhibition on chitin biosynthesis that only exists in insect cuticle and fungal cell wall but is absence in mammals and higher plants. Therefore, it possesses high efficiency, low toxicity, and safety for non-target organisms. These advantages accord with the requirement of the green pesticide. In this review, the discovery of leading product, structural modification, structure-activity relationships, and the action mechanism of etoxazole analogues, are summarized comprehensively. It is expected to provide fundamental support for the development of novel acaricidal/insecticidal compounds.