Studies on Antiatherosclerotic Agents. Synthesis of 7-Ethoxycarbonyl-4-formyl-6, 8-dimethyl-1(2H)-phthalazinone Derivatives and Related Compounds

Abstract

Derivatives of 7-ethoxycarbonyl-4-formyl-6, 8-dimethyl-1(2H)-phthalazinone and closely related compounds were synthesized using Wittig and epoxidation reactions. Ring opening amination of the epoxides were carried out using dimethylaluminum amide reagents under mild reaction conditions. β-Keto ester and β-diketone moieties were introduced through diazo derivatives. These moieties were reacted with hydrazine hydrate to produce 4-pyrazolyl derivatives.The derivatives were tested for their inhibitory effect on platelet aggregation, and their relaxing effect on blood vessels.