| Sythesis of ticargrelor has attracted widespread attention of chemists as ticargrelor is the mainstream product in the market of anticoagulants. From those synthetic routes published, we can see three main intermediates that include 4, 6-dichloro-2-(proylthio)-pyrimidin-5-amine,(1S,2R,3S,4R)-1-(2-hydroxyethoxy)-2,3-O-isopropyl-idene-4-amino-1,2, 3-cyclopentanetriol and(1R,2S)-2-(3,4-difluorophenyl) cyclol-anamine. There is the possibility of improvement of synthetic approach and market requirement for the three intermediates. In this thesis, we try to improve and find new synthetic routes for the intermediates of 4,6-dichloro-2-(propylthio)-pyrimidin-5-amine and(1S,2R,3S,4R)-1-(2-hydroxyethoxy)-2, 3-O-isopropylidene-4-amino-1,2,3-cyclopentanetriol, and some related methodology also has been studied. This thesis included the following six chapters:Chapter 1: This chapter gave a brief introduction for thrombotic diseases, anticlotting drugs and ticagrelor.Chapter 2: Through analysis and comparison from reported the synthetic routes about the intermediate 4,6-dichloro-2-(propylthio)-pyrimidin-5-amine, we designed a new synthetic route to innovate and optimize the synthetic method.Chapter 3: From the intermediate 4,6-dichloro-2-(propylthio)-pyrimidin-5-amine innovation and optimization, we found the synthetic methods of thiobarbituric acid derivatives in present and then we innovated and optimized them.Chapter 4: From the intermediate 4,6-dichloro-2-(propylthio)-pyrimidin-5-amine innovation and optimization, we found the synthetic methods of nitro compounds in present and then we studied using metal nitrates in the single nitration of phenol compounds.Chapter 5: Through analysis and comparison from the synthetic routes about the intermediate(1S,2R,3S,4R)-1-(2-hydroxyethoxy)-2,3-O-isopropylidene-4-amino-1,2,3-cyclopentanetriol, we designed a new synthetic route to innovate and optimize the synthesis method.Chapter 6: It showed the summary and outlook... |
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