Studies on antiatherosclerotic agents. Synthesis of 7-ethoxycarbonyl-4-formyl-6,8-dimethyl-1(2H)-phthalazinone derivatives and related compounds.
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.
Eguchi
Y
Y
Institute for Medical and Dental Engineering, Tokyo Medical and Dental University, Japan.
Sasaki
F
F
Takashima
Y
Y
Nakajima
M
M
Ishikawa
M
M
D000818:Animals; D001161:Arteriosclerosis / Q000188:drug therapy*; D010793:Phthalazines / Q000138:chemical synthesis* / Q000494:pharmacology; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D051381:Rats
D010793:Phthalazines; D010975:Platelet Aggregation Inhibitors