A Convenient Synthesis of N', N'-Disubstituted N-Fluorophenylformamidines by Using Microwave and Their Insecticidal Activities

Phenylformamidine derivatives are well known as insecticides for their specific activity against the insects. It has now been established that they show insecticidal activity as agonists on the octopamine receptor which is located in the synapse membrane. The reaction of triethylorthoformate and fluoroanilines gave formimidates (1) in good yields and N',N'-Disubstituted N-fluorophenylformamidine derivatives were synthesized more easily by using microwave. This microwave reaction condition gave products in high yields and faster reaction time than conventional methods. All the compounds were screened for their biological activity agaist harmful insects of plant hoppers, moths, aphids and mites. Synthetic compounds of 2-I-a, 2-I-c, 2-I-d, 2-II-d showed good activity against mites and plant hoppers.