Aniline → 3-Phenylquinazolinone

Participants

Reaction Steps

The quinazolinone inhibitors (e.g., inhibitor compound formula D) of the general structure 16 (Scheme 4, below) are made in two steps from the commercially available benzoxazine 12 (Scheme 4). The benzoxazine is first heated with an aniline (13) to form 3-phenylquinazolinone derivative 14. This intermediate is then reacted with substituted furan-2-carboxaldehyde 15 in the presence of sodium acetate (NaOAc)/acetic acid (AcOH) to provide the desired quinazolinones 16.

Provenance & Evidence