Anti-platelet Drugs Pa, And Gray And Its Derivatives Synthesis Research

The process of anti-platelet agent Paraicogrel was studied in this paper, the design and synthesis of its derivatives were reported as well.The development of anti-platelet agents was described in this paper. Pamicogrel, a new anti-platelet drug, was introduced in detail, including its pharmacokinetics and pharmacodynamics. The process of Pamicogrel was researched particularly. With 4-methoxyl-benzaldehyde , ethyl chloroformate , potassium thiocyanate as the starting materials, it had been prepared in a seven-step procedure , which was benzoin condensation, hydrolysis and alkylation with PTC et al, in overall yield of 38. 1%.Based on the analysis of structure-activity relationships(SAR) of Pamicogrel analogues, six target compounds were designed and prepared, five of them were new compounds. The structures of Pamicogrel and its derivatives were confirmed by H-NMR, IR, MS.The inhibitory activity of anti-platelet aggregation of three compounds against rabbits in vitro were tested. The preliminary result showed that three compounds had anti-platelet aggregation activities.