The 2-(2-arylmorpholino)ethyl esters of naproxen were designed and synthesized according to the structure-activity relationship by the reaction of 2-aryl-4-(2-hydroxyethyl)morpholine with 2-(6-meth-
oxy-2-naphthyl)propionyl chloride in yields of 24.2%～76.5%. 2-Aryl-4-(2-hydroxylethyl)morpholine intermediates were synthesized from arylethanones by bromination, amination and deoxidization. Their structures were confirmed by 1H NMR. The preliminary bioassays indicated that compound 1d exhibited a 96.32% inhibition rate against COX-2 in vitro at 10 μmol/L.

Key words: naproxen, cyclooxygenase-2, inhibitor, morpholine derivative, synthesis