Expedient Synthesis of 6‐Functionalized Azabicyclo[4.1.0]heptane Derivatives

An efficient approach to the synthesis of previously unreported azabicyclo[4.1.0]heptane‐derived building blocks is reported following the divergent strategy. The common synthetic precursor – tert‐butyl 6‐(hydroxymethyl)‐3‐azabicyclo[4.1.0]heptane‐3‐carboxylate was obtained in four steps with 38 % overall yield and was involved in short reaction sequences (1–3 steps) to provide the target bifunctional derivatives, including novel bicyclic N‐Boc protected γ‐amino acid. The described compounds are interesting in terms of lead‐likeness concepts, according to which the rigid 3D‐shaped and sp³‐enriched frameworks are among the most promising entry points for drug discovery projects.