Preparation method of platelet aggregation inhibitor ticagrelor

The invention discloses a preparation method of platelet aggregation inhibitor ticagrelor, and belongs to the field of drug synthesis. According to the method, a compound 2 and a compound 3 are used as raw materials, substitution reaction, cyclization reaction, amination reaction and deprotection ar...

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Hauptverfasser: YIN MENGJUAN, SU FUYING, GUAN YUQING, ZHANG YUNQIAO, LIU YUXIA, HAO ERJUN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of platelet aggregation inhibitor ticagrelor, and belongs to the field of drug synthesis. According to the method, a compound 2 and a compound 3 are used as raw materials, substitution reaction, cyclization reaction, amination reaction and deprotection are sequentially carried out, a crude product is recrystallized by ethyl acetate and normal hexane toobtain the ticagrelor, and the purity of the ticagrelor is up to 99.5% or above. Compared with methods reported in existing literatures, the method has the advantages that the reaction route is obviously shortened, the process stability is high, use of toxic solvents and high-pollution reagents is avoided, and the method is relatively more environmentally friendly and suitable for large-scale production. 本发明公开了一种血小板聚集抑制剂替格瑞洛的制备方法,属于药物合成领域。以化合物2和化合物3为原料,依次经过取代反应、关环反应、氨基化反应和脱保护后,粗产物经过乙酸乙酯和正己烷重结晶后,得到替格瑞洛,纯度高达99.5%以上。相比现有文献报道的方法,反应路线明显缩短,工艺稳定性高,避免了有毒溶剂和高污染试剂的使用,相对更加绿色环保,适合大规模化生产。