A Convenient and efficient method for the preparation of 6-Acyl-2(3H)-benzoxazolones

Benzoxazolinone derivatives have been found to exhibit various pharmacological properties and 6-acyl-2(3H)-benzoxazolones are considered as key starting materials for the preparation of these compounds. Reported here are the optimal conditions for a regioselective acylation at the 6-position of the benzoxazolinone ring. A general method leading to the expected products in excellent yields consists in using a mixture of aluminum chloride-dimethylformamide as catalyst and acid anhydrides or chlorides as acylating agents.