Studies On The Synthetic Technology Of TXA₂ Synthetase Inhibitor Ozagrel

The pharmacological mechanism of thrombus and the development of antithrombotic drugs were described in this paper. The pharmacological action and pharmacokinetics of TXA₂ (ThromboxaneA₂) synthetase inhibitor Ozagrel were introduced particularly.The three synthetic routes of Ozagrel of literature were investigated after the theoretical analyzing. The two routes were chosen as the object of technologic studies. The other two new synthetic routes were designed. After the detailed investigation about four synthetic routes, The better route was determined as for the goal of higher yield, lower cost and simplified procedure, the target compound Ozagrel was obtained from p-methyl benzaldehyde and imidazole which were the raw materials, and was synthesized through 8-step synthetic reactions. The overall yield has been increased to 35.4%, which was 19.1% more than that of the original literature method.By the experimental uniform design, the synthetic process of (E) -3-(4-methylphenyl)-2-propenoic acid and (E)-3-[4-(1H-Imidazol-1-ylmethyl)phenyl]-2-propenoic ester was modified. Several factors of those reactions were investigated, such as phase transfer catalyst, solvent, reaction time, reaction temperature. So a more suitable technology to industrialization was found.