1,1,1,3,3,3-Hexafluoroisopropanol (HFIP) Promoted N-Alkylation of Quinazolinones through Nucleophilic Substitution of Benzyl Alcohols

J Org Chem. 2023 Oct 6;88(19):14189-14192. doi: 10.1021/acs.joc.3c01366. Epub 2023 Sep 22.

Abstract

We describe here a protocol for alkylation of quinazolinones with a series of primary or secondary alcohols under metal-free conditions. A class of quinazolinone derivatives were obtained in 31%-97% yield with good functional group tolerance. This protocol provides chemists a direct and effective way to obtain bioactive quinazolinone derivatives.