摘要 |
<p>NEW MATERIAL:A compound shown by formula I (R is lower alkyl or methoxy; n is 0-2; pyridine is bonded at 2-, 3- and 4-positions). EXAMPLE:1-(4-Tolyl)-4-(3-pyridyl)phthalazine. USE:An inhibitor of blood platelet aggregation. Showing low toxicity and high activity and useful for preventing and treating cerebral thrombosis, cerebral infarct, peripheral arterial atresia, etc. PREPARATION:A phenyl derivative shown by formula II as a starting substance is subjected to Friedel-Crafts reaction, a Grignard reagent is reacted with pyridinealdehdye to give a compound shown by formula III. Then the hydroxy group is oxidized to give a ketone derivative and protecting group of carbonyl group is removed to give a compound shown by formula IV. Further the compound shown by the formula IV is subjected to ring closure with hydrazine to give a compound shown by formula I.</p> |