Studies on antiatherosclerotic agents. Synthesis of 7-ethoxycarbonyl-4-formyl-6,8-dimethyl-1(2H)-phthalazinone derivatives and related compounds

Chem Pharm Bull (Tokyo). 1991 Mar;39(3):795-7. doi: 10.1248/cpb.39.795.

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. beta-Keto ester and beta-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.

MeSH terms

  • Animals
  • Arteriosclerosis / drug therapy*
  • Phthalazines / chemical synthesis*
  • Phthalazines / pharmacology
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Rats

Substances

  • Phthalazines
  • Platelet Aggregation Inhibitors