Synthesis of New Aryl(Hetaryl)-Substituted Tandospirones Under Reductive Heck Type Hydroarylations and Isoxazoline Derivatives via 1,3-Dipolar Cycloaddition Reactions with Expected Anxiolytic Activity

Abstract

The C-C coupling of bicyclic alkene 4 with aryl and heteroaryl iodides gave under reductive Heck conditions the Caryl(hetaryl), N-[((4-pyrimidin-2-yl) piperazin-1-yl) butyl] substituted bicyclic imides 5a-f. The [3+2] cycloadditions of 4 with various nitrile oxides yielded the bridged isoxazoline derivatives 6-8 with potential biological activity.