Study On The Synthesis Of The Key Intermediates Of Ticagrelor

Ticagrelor is a new and selective small molecule anticoagulants developed by AstraZeneca. As a new generation of anticoagulants, ticagrelor is popular because of its significant efficacy and low side effect. It has a good market prospects as well as a broad space about the process research. Since then, the study of the synthesis of ticagrelor is of great significance.This thesis mainly includes the optimization of the synthetic route of three key intermediates. The original synthetic routes of ticagrelor intermediates are complex and with low yield, the start materials are expensive and some of the solvents are toxic. So the original synthetic routes are not suitable for industrial production.This study mainly focus on improvement of synthetic route according to the reports in literatures. Replacing some of the high toxic solvents and expensive reagents by low toxicity and cheap reagents, which make it available to industrial production. Some reactions were optimized and some of the complex operations were simplified to improve the efficiency while the costs can be greatly saved. The starting materials of three intermediates are cheap and commercial available, and reaction conditions were mild. The purity of all the three final products is more than 99%. The operation of the synthetic route is simplified, which makes it possible for the industrial production of ticagrelor intermediates.