Antithrombotic Drugs - The Synthesis Process Of The Prasugrel Study

Prasugrel, a new generation of oral anti-platelet aggregation drugs which was co-developed by Lilly and Sankyo, has the merits of high oral bioavailability, instant effect and loading doses free when using in the treatment of atherosclerotic disease and acute coronary syndrome.The present thesis firstly reviewed the existing synthetic routes and reaction conditions of Prasugrel. Then we designed a simple and convenient synthetic route using inexpensive and facile starting materials and reagents in consideration of industrial production. Two key steps of the route were modified. The first was one-pot synthesis of Prasugrel and the other was the synthesis of 2-bromo-l-cyclopropyl-2-(2-fluorophenyl)ethanone with a new method. Our investigation suggested that the modification of the synthetic route provide several advantages, including high overall-yield (yield was improved 14.6% to 19.7%), easy-work up, and avoiding the use of chromatography for purification.