Synthesis process of Ticagrelor intermediate

The invention discloses a synthesis process of a Ticagrelor intermediate, and belongs to the technical field of medicine synthesis. A compound I is prepared by using hydroxylamine hydrochloride and benzyl chloroformate as raw materials; the compound I and cyclopentadiene react to obtain a compound I...

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Bibliographische Detailangaben
Hauptverfasser: LIU BIN, SUN CHAO, XU HUAFENG, QIAO MINGFU, DOU ZHENGUO
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The invention discloses a synthesis process of a Ticagrelor intermediate, and belongs to the technical field of medicine synthesis. A compound I is prepared by using hydroxylamine hydrochloride and benzyl chloroformate as raw materials; the compound I and cyclopentadiene react to obtain a compound II; finally, dihydroxylation is performed to obtain a compound III. The synthesis process is simple and efficient, and has the advantages that the raw materials are cheap and can be easily obtained; the process can be easily monitored; the conditions are mild; the operation is simple; the yield is high. The synthesis process is suitable for industrial large-scale production. 本发明公开了种替格瑞洛中间体的合成工艺,属于药物合成技术领域。本发明以盐酸羟胺和氯甲酸苄酯为原料,制得化合物I,再与环戊二烯反应得到化合物II,最后双羟基化得到化合物III。本发明的合成工艺简单高效,具有原料廉价易得、过程易监控、条件温和、操作简单、收率高的优点,更适合工业大规模生产。