Design, Synthesis, and Insecticidal Evaluation of Neonicotinoid Analogues With 1,2‐Dihydropyridine Scaffold

A series of neonicotinoid analogues with 1,2‐dihydropyridine scaffold were synthesized by the novel annulation reaction. Bioassay indicated that some compounds exhibited good insecticidal activity against Aphis craccivora at a concentration of 100 mg/L, and the substituents on the phenyl group have a great influence on insecticidal activity. Especially, the LC 50 values of compounds A3 and A19 were 17.089 and 4.792 mg/L, respectively. Molecular docking results revealed that compound A19 bound to Lymnaea stagnalis acetylcholine binding protein via H‐bonds with the residues of Leu102, Val114, and Arg55. These results proposed a promising guide for the design of neonicotinoid analogues with 1,2‐dihydropyridine scaffold.