Study On Synthesis Procedure Of Anti-platelet Aggregation Drugs Prasugrel

In recent years, cardiovascular morbidity shows ascendant trend, cardiovascular disease has serious harm to human health, it is the current cause deformity and death the chief factor, and platelet inhibitors can effectively improve and prevention of cardiovascular disease, therefore platelet inhibitors research has become the hotspot of cardiovascular disease treatment.A new generation of platelet P2Y12 blocker prasugrel, which compares more quickly and more effectively inhibiting platelet aggregation with present best-selling thiazide chlorine and clopidogrel. it`s a precursor drug, ticlopidine and clopidogrel`s analogues, which formed a active molecule after metabolic in the body, combining with platelet P2Y12 receptors and play antiplatelet agglomerate activity. This paper reviewed the development of platelet inhibitors, and antiplatelet condensed drug prasugrel synthetic process of study, at the same time for the clinical application prospect. 2-oxo-2, 4, 5, 6, 7, 7a–hexahydrothieno [3, 2 -c] pyridine hydrochloride was prepared from 4, 5, 6, 7- tetrahydrothieno [3, 2- c] pyridine hydrochloride via amino protection,oxidation and remove amino protection foundation .The reaction of the Grignard reagent prepared from 2-fluorobenzyl bromide and Mg in ether with cyclopropyl cyanide gave cyclopropyl-2-fluorobenzyl kotone, which was brominated with NBS in CHCl3 to getα-cyclopropyl carbonyl-2-fluorobenzyl bromide. In alkaline environment,α-cyclopropyl carbonyl-2-fluorobenzyl bromide is reacted substitution nucleophilic reaction with 2-oxo-2, 4, 5, 6, 7, 7a-hexahydrothieno[3, 2-c] pyridine hydrochloride and then via acetylation reaction to get prasugrel with yield of 21.8%.