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2-Boc-2,6-diazabicyclo[3.2.0]heptane is a useful reagent for the preparation of pyrimidine derivatives as KRas G12C inhibitors for treatment of KRas-mediated diseases.

The synthesis of the 2,6-diazabicyclo[3.2.0]heptane scaffold, which comprises a fused azetidine and pyrrolidine system, typically employs an intramolecular photochemical [2+2] cycloaddition as the key ring-forming step. This reaction is performed on a protected N-vinyl-β-lactam or a related unsaturated diamide, in which the vinyl group and a tethered alkene are positioned to form the strained cyclobutane ring of the azetidine moiety upon irradiation. Subsequent deprotection of the nitrogen atoms (e.g., Boc or Cbz removal) yields the free diamine.