Synthesis of 1,3-Diazetidin-2-ones (Aza-β-lactams) as Rationally Designed Transpeptidase and β-Lactamase Inhibitors

Article abstract of DOI:10.1016/0040-4039(95)01473-U

Pyrimidinone 4 is converted to diazetidinone carboxaldehyde 6.Selective chemical transformations on tricarbonyl substrate 6 with different reagents are performed.Synthon 6 is employed as a versatile template for elaboration to bicyclic diazetidinones 7, 12 and 15.A novel class of aza-β-lactam compounds are synthesised as potential transpeptidase and β-lactamase inhibitors.