Base-Catalyzed, Solvent-Free Synthesis of Rigid V-Shaped Epoxydibenzo[ b, f][1,5]diazocines

J Org Chem. 2021 Jul 2;86(13):8955-8969. doi: 10.1021/acs.joc.1c00884. Epub 2021 Jun 23.

Abstract

A novel method for the synthesis of epoxydibenzo[b,f][1,5]diazocines exhibiting a V-shaped molecular architecture is reported. The unique approach is based on unprecedented base-catalyzed, solvent-free autocondensation and cross-condensation of fluorinated o-aminophenones. The structure of the newly synthesized diazocines was confirmed independently by X-ray analysis and chiroptical methods. The rigidity of the diazocine scaffold allowed for the separation of the racemate into single enantiomers that proved to be thermally stable up to 140 °C. Furthermore, the inertness of the diazocine scaffold was demonstrated by performing a series of typical transformations, including transition metal-catalyzed reactions, proceeding without affecting the bis-hemiaminal subunit.