1,2-Benzisoxazoles are motifs present in a wide range of pharmaceutically potent agents, including diuretics, 1 acetylcholinesterase inhibitors, 2 antileptics, 3 and neuroleptics. 4 As a result, several approaches have been developed to obtain these heterocycles. 5 Despite the diversity of existing methods only two are frequently used to access 3-substituted-1,2-benzisoxazoles (Fig. 1). ... Synthetic routes to 1,2-benzisoxazoles. Synthetic routes to 1,2-benzisoxazoles.