The application provides a 1-heteroaryl-3-
sulfone group bicyclo[1.1.1]
pentane compound and a preparation method and application thereof, and belongs to the technical field of synthesis of pharmaceutical intermediates. The compound provided by the application is a double-substituted bicyclo[1.1.1]
pentane containing a
sulfone group and a heteroaryl group and derivatives thereof, wherein the
sulfone group is an important
pharmacophore, plays a role in antitumor drugs by participating in
hydrogen bond interaction, regulating
cell signaling pathways and the like, and the series of compounds have
antitumor activity. The application uses cheap and easily available
sulfonic acid chlorides, [1.1.1]spiro
propeller and heteroaromatic compounds as raw materials, and prepares a series of sulfone group and heteroaryl group double-substituted bicyclo[1.1.1]
pentane under mild conditions through a three-component tandem reaction with
high selectivity and high yield, and the preparation method is simple and suitable for industrial production.