| Cangrelor,which is a novel anti-platelet injective drug and belonges to the small molecule inhibitors of platelet P2Y12,was first developed by Astrazeneca Company then transferred to Medicines Company for post-development.It was marketed in the United States after being approved by the FDA in 2015.It is mainly used to the patients who need to receive percutaneous coronary intervention.With rapid onset,high activity,good effect and so on,Cangrelor which reversibly inhibit ADP-induced platelet aggregation will reduce the risk of thrombotic cardiovascular disease.Therefore,Cangrelor has great prospect in clinics.The structure of Cangrelor,similar to adenosine triphosphate,is mainly composed of two parts.One part is the nucleus of adenosine 6-N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)mercapto]-adenosine and the other is phosphoric acid side chain moieties.In this paper an industrially efficient new route for manufacturing the former,which is a key intermediate of Cangerlor,is obtained by nine-step chemical reactions by starting from ethyl cyanoacetate.After lots of experimental explorations,the optimal process for6-N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)mercapto]-adenosine was reached.Compared with the reported articles,the route has advantage of low cost,mild conditions and industrially feasible.MS and ~1H NMR were used to characterize the target of molecule of 6-N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)mercapto]-adenosine and intermediates.. |
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