The Synthesis Of Novel TXA₂/PGH₂ Receptor Antagonist CV-4151 And Its Analogues

The advance of the anti-platelet agents of CV-4151 was reviewed in this paper. A new TXA2/PGH2 receptor antagonist CV-4151 was briefly introduced about its pharmacological properties.The synthetic routes of CV-4151 were studied and the total yield of 9 steps amounted to 16. 2%. The structure was elucidated through physic-chemical properties and spectroscopic analyses. Meanwhile, the synthetic method of co-bromocaproic acid was simplified and improved.In addition, the structure-activity relations of TXA2/PGH2 receptor antagonist CV-4151 were summed up. Based upon it, four compounds were designed and synthesized. S02, SO3 and S04 have not been reported in literature.The inhibitory activities of anti-platelet aggregation of all compounds by rabbits in vitro were tested .The preliminary result showed that CV-4151 and some analogues had perfect anti-platelet aggregation activities.