Preparation of Quinazolinoquinazolinones via a Cascade Approach

J Org Chem. 2018 Nov 16;83(22):14138-14145. doi: 10.1021/acs.joc.8b02239. Epub 2018 Nov 1.

Abstract

A one-pot synthesis of quinazolino[3,4- a]quinazolin-13-ones was realized from the direct reaction of o-(methoxycarbonyl)benzenediazonium salts, nitriles, and 2-cyanoanilines in moderate to good yields. This method utilizes the in situ generation of reactive N-arylnitrilium ion, which undergoes further amination/tandem cyclization/amidation to deliver the desired polycyclic scaffolds with consecutive formation of four N-C bonds. Flexibility in substitution patterns, mild reaction conditions, and operational simplicity are the salient features of this methodology.

Publication types

  • Research Support, Non-U.S. Gov't