Abstract 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 ...