Preparation method of oseltamivir

The invention provides a preparation method of oseltamivir, the method does not need to use noble metal to catalyze and remove a protecting group on nitrogen, the reaction condition is mild, the operation is simple and convenient, the steps are few, the cost is low, the yield is high, (1aR, 5aR, 5R)...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: FENG WENCHAO, ZHANG XINGXIAN, QIAN HONGJIE
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention provides a preparation method of oseltamivir, the method does not need to use noble metal to catalyze and remove a protecting group on nitrogen, the reaction condition is mild, the operation is simple and convenient, the steps are few, the cost is low, the yield is high, (1aR, 5aR, 5R)-1-(2-methylpropyl-2-yl)-5-(1-ethylpropoxy)-1a, 2, 5, 5a-tetrahydrobenzo [1, 2] aziridine-3-ethyl formate is used as an initial raw material, and the preparation method is simple and convenient to operate and high in yield. The preparation method comprises the following steps: carrying out ring opening and N-acetylation reactions, and finally removing tert-butyl and p-methoxybenzyl protecting groups to prepare oseltamivir. 本发明提供一种奥司他韦的制备方法,该法不需要使用贵金属催化脱除氮上保护基,反应条件温和、操作简便、步骤少、成本低、收率高,该法以(1aR,5aR,5R)-1-(2-甲基丙-2-基)-5-(1-乙基丙氧基)-1a,2,5,5a-四氢苯并[1,2]氮杂环丙烷-3-甲酸乙酯为起始原料,经历开环、N-乙酰化反应,最后脱除叔丁基和对甲氧基苄基保护基,制得奥司他韦。