Chemo-, regio-and diastereoselective approach to the synthesis of arylmethylideneimidazothiazolotriazines has been developed based on the Michael addition/retro-Michael reaction and Michael addition/retro-Michael reaction/skeletal rear-rangement cascade processes in the reactions of imidazo [4,5-e] thiazolo [3,2-b] [1,2,4]triazines with arylmethylidene derivatives of malononitrile.