Facile Synthesis of 2-Aminocyclobutenylphosphonates

Abstract

The addition of various amines to diethyl 4-chlorobut-1-yn-1-ylphosphonate produced novel biologically potent substituted diethyl 2-aminocyclobut-1-en-1-ylphosphonates in 70–83% isolated yield. This regioselective reaction was carried out at room temperature in the absence of solvent and catalyst.