332047-13-9Relevant articles and documents
A oseltamivir acetyl aziridine intermediate preparation method
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Paragraph 0033; 0034; 0035, (2018/09/21)
The invention discloses a oseltamivir (Oseltamivir) acetyl aziridine intermediate I (Figure 1) of the preparation method. In the method of the shikimic acid epoxy derivative II as raw materials, by the six chemical synthesis step (Figure 2) to make the oseltamivir acetyl aziridine intermediate I, yield is 44 - 61%. The invention comprises the following six chemical synthesis steps: (1) epoxy compound II of the 3 - position open-loop and through the one-pot three-step series formed by the reaction of 3, 4 - bit aziridine compound III; (2) 3 - pentanol selective attack 3 - bit open-loop to obtain compound IV; (3) 4 - bit removing allyl get compound V; (4) 4 - amino acetylation to obtain compound VI; (5) 5 - hydroxy methyl sulfonylation to obtain compound VII; (6) 4 - acetyl amino attack at the 5 - position of the ring to obtain the oseltamivir acetyl aziridine intermediate I.
