We have developed a solid-phase synthesis of 1,2,3-benzotriazin-4-ones through cyclization of 2-aminobenzamides via diazotization. The development of an efficient synthesis is important from the viewpoint of drug discovery, considering the various bioactivities of these derivatives. The precursors of 1,2,3-benzotriazin-4-ones, 2-aminobenzamides, were prepared from solid-supported amines and 2-nitrobenzoic acids. Various 1,2,3-benzotriazin-4-ones were obtained with high purity using SynPhaseTM Lanterns.
solid-phase synthesis; drug; quinazoline; 1,2,3-benzotriazin-4-one; SynPhaseTM Lantern; diazotization