Synthesis of C3-halo substituted bicyclo1.1.1pentylamines via halosulfoamidation of 1.1.1propellane with sodium hypohalites and sulfonamides

摘要

Herein, we report a catalyst-free synthesis of C3-halo substituted bicyclo[1.1.1]pentylamines under mild conditions. The reaction involves the use of sodium hypohalites and sulfonamides to generate N-halosulfonamides in situ, which subsequently undergo radical addition with [1.1.1]propellane to yield the desired products with suitable functional group tolerance.