Sulfamide instead urea in Biginelli reaction: from black box to reality

The scope and limitation of classical Biginelli reaction expanded to principally novel substrates: sulfamide and its monosubstituted analogues. The preparative procedure was optimized. The reasons for the unavailability of such compounds earlier were determined. The relationship between the structure and stability of final compounds and the nature of starting materials were detected. Some mechanistic observations were shown and discussed. The prospects for employing these compounds for new 3D-shape MedChem relevant libraries were disclosed.