Abstract: The discovery of pesticides with novel mode of action is crucial for modern crop protection. In present work, a series of novel piperidin-4-ol derivatives were synthesized by 5-step reactions using piperidinol and catechol as starting materials. All target compounds were characterized by ¹H NMR, ¹³C NMR and HRMS. The biological activities of synthesized compounds were evaluated against Meloidogyne incognita and Pseudaletia separata Walker respectively. It was found that some target compounds exhibited good nematicidal activity against M. incognita at 25 mg/L. Obvious weight reduction on P. separata was also observed for most of the compounds at 500 mg/L due to their anti-feeding effects on the armyworm.