Design and synthesis of dihydroisoquinolones for fragment-based drug discovery (FBDD)

This study describes general synthesis aspects of fragments for FBDD, as illustrated by the dihydroisoquinolones 1–3. Previous Rh(III) methodology is extended to incorporate amines, heteroatoms (N and S), and substituents (halogen, ester) as potential binding groups and/or synthetic growth points for fragment-to-lead elaboration.