What do FDA approved drugs propranolol, naproxen and terbinafine have in common? They all contain a naphthalene moiety, which is a common structural motif in biologically active compounds. The reasons are perhaps clear to most medicinal chemists. Naphthalene fits well into many lipophilic pockets on proteins, many functionalized derivatives of naphthalene are commercially available and…
Top notch medchem building blocks got unlocked. Chemists from Enamine Ltd. published a robust route to saturated azabicyclic scaffolds (Angewandte Chemie): “𝘉𝘪𝘤𝘺𝘤𝘭𝘪𝘤 𝘐𝘴𝘰𝘴𝘵𝘦𝘳𝘦𝘴 𝘰𝘧 𝘗𝘺𝘳𝘪𝘥𝘪𝘯𝘦/𝘗𝘪𝘱𝘦𝘳𝘪𝘥𝘪𝘯𝘦: 𝘍𝘳𝘰𝘮 𝘚𝘺𝘯𝘵𝘩𝘦𝘴𝘪𝘴 𝘵𝘰 𝘈𝘱𝘱𝘭𝘪𝘤𝘢𝘵𝘪𝘰𝘯𝘴” Key innovationKOtBu/I₂/CO₂-mediated cyclization of cyclic alkenyl amines, delivering:✔️ 2-azabicyclo[2.2.2]octanes (35-73% yield)✔️ 2-azabicyclo[3.2.1]octane (69% yield)✔️ 2-azabicyclo[2.2.1]heptanes (75-85% yield)✔️ 7-azabicyclo[2.2.1]heptane (70% yield)✔️ 2-azabicyclo[3.1.1]heptanes (62-73% yield)✔️ 2-azabicyclo[2.1.1]hexanes (52-90% yield) ✅ 52–90% yield✅ Scales up to…