Development of one-pot three component reaction for the synthesis of N′-aryl-N-cyanoformamidines, essential precursors of formamidine pesticides family

Efficient one-pot three component reaction of aniline derivatives with cyanoamide and triethyl orthoformate at reflux in toluene affords N′-aryl-N-cyanoformamidines in high yields just by the distillation of the azeotrope toluene/ethyl alcohol. Labelled d9-Amitraz is prepared by the application of this procedure in the synthesis of formamidine pesticides family.