“…Hence, great efforts have been made to synthesize 1,2-benzisoxazoles, driven in part by the expected biological activities. In general, the reported synthesis of 1,2-benzisoxazoles could be found utilizing five distinct approaches (Scheme ): (1) [3 + 2]-cycloaddition of in situ generated nitrile oxides to arynes; , (2) catalyzed cyclodehydration of 2-hydroxyaryl aldoximes and ketoximes; (3) catalyzed intramolecular nucleophilic substitution of oximes in the presence of strong bases; (4) palladium-catalyzed intermolecular [4 + 1]-annulation of N -phenoxy acetamide with aldehydes; (5) intramolecular cycloaddition of S N Ar products from fluorous oxime tags or polymer-bound oximes to o -fluoro-benzonitriles . Yet, some limitations and drawbacks of these approaches could still be found such as the requirement of 3–4 steps for most reported procedures, preparation of starting materials or a long reaction time, , formation of undesirable byproducts, , and some harsh reaction conditions such as a strong base in the substitution of aryl halides. ,, …”