Diastereoselective synthesis of highly functionalized polycyclic benzosultams via tandem cyclisations of cyclic N-sulfonylimines with in situ generated Huisgen 1,4-dipoles

Abstract

Under mild reaction conditions, the tandem cycloadditions of cyclic N-sulfonylimines with in situ generated Huisgen 1,4-dipoles from dialkyl acetylenedicarboxylates and pyridines underwent readily, and delivered highly functionalized polycyclic 1,2,3,4-tetrahydropyrimidine-fused benzosultams in low to excellent chemical yields with excellent diastereoselectivities.