https://hal.archives-ouvertes.fr/hal-03416913/document

Modular Approach to Substituted Pyridoazepinones.

The synthesis and preliminary ADME evaluation of ­novel 4-(trifluoromethyl)-5,7,8,9-tetrahydro-6H-pyrido[3,2-b]azepin-6-ones is presented. The key step is a ring expansion of 4-(trifluoromethyl)-7,8-dihydroquinolin-5(6H)-ones via a Beckmann rearrangement. The rearrangement opens up possibilities to access novel unexplored scaffolds for medicinal chemistry. The biopharmaceutical profiling revealed a strong structural dependency of the druglike properties.

Hans Loones

Papers

Synthesis and early ADME evaluation of a novel scaffold, tetrahydro-6H-pyrido[3,2-b]azepin-6-one