A simple and efficient method for the synthesis of 1,2-benzisoxazoles:A series of its potent acetylcholinesterase inhibitors

摘要

A simple and efficient method for the synthesis of 6-fluoro-3-(4-piperidinyI)-l,2-benzisoxazole hydrochloride is achieved.This reaction involves hydroxylamine sulfate/ KOH mediated,in situ generated oxime formation and its subsequent internal cyclisation followed by alkaline hydrolysis of N-protected ketone in one step.Synthesis of 1,2-benzisoxazole analogues is described and they are found to be potent acetylcholinesterase inhibitors.