A new synthesis of N‐substituted‐2‐alkyl(or aryl)quinazolin‐4‐amines by amide base‐mediated cyclization of carbox‐imidamides derived from 2‐(trifluoromethyl)benzenamine

Abstract

A one‐pot preparation of carboximidamides (amidines) 11–14 involves treatment of amides 2–5 with phosphorus pentachloride followed by the treatment of the resultant crude imidoyl chlorides 7–10 with ammonia. Amidines 11–14 are cyclized to quinazolines 20–26 in lithium alkylamide‐or dialkylamide‐mediated reactions.