Derivatives containing the thieno [2,3-d]pyrimidin-4-one system, potential selective COX-2 inhibitors, were prepared starting from ethyl ester of 2-isothiocyanato-5-phenyl-3-thiophenecarboxylic acid (2); their structural elucidation is also reported.J. Heterocyclic Chem., 40, 869 (2003).Derivatives containing the thienopyrimidine systems are reported to possess several important pharmacological properties [1]; in particular some derivatives of the 6-showed interesting anti-inflammatory and analgesic activities without ulcerogenic activity and with low acute toxicity.Recent developments in the research of non-steroidal anti-inflammatory drugs (NSAIDs) as selective inhibitors of COX-2 [3,4] have prompted us, on the basis of the above heterocyclic system [2] and structures of leads [3,4], to prepare new derivatives with the characteristic functional groups of selective COX-2 inhibitor drugs.In this paper we report the synthesis and the structural elucidation of a series of new derivatives containing the 6-phenyl-thieno[2,3-d]pyrimidin-4-one heterocyclic system as a stage of research of compounds with effective analgesic and anti-inflammatory activities as selective COX-2 inhibitors.The key compound was the ethyl ester of 2-isothiocyanato-5-phenyl-3-thiophenecarboxylic acid (2) prepared, without the production of pollutants, in acetone at room temperature from the reaction of amino ester 1 and thiophosgene with subsequent dilution in water (Scheme 1). The reaction at room temperature with hydrazine or with mesylhydrazine and treatment of the resulting