Synthesis of 3D-enriched macro- or polycyclic ligands, F. Hausch

Synthesis of 3D-enriched macro- or polycyclic ligands

Challenging drug targets such as FKBP51 are difficult to address with small molecules present in typical screening libraries. For our most promising compounds it has been detrimental to explore novel chemotypes such as C5-subsituted aza-amide bicycles. Access to this novel scaffold was enabled by the development of concise syntheses featuring powerful state-of-the-art transformations such as cross-metathesis, TMS-assisted acyl-iminium cyclization, sp2-sp3 Negishi coupling, or asymmetric Shi epoxidation.

Bild: F. Hausch