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METHOD FOR PREPARING LANINAMIVIR OCTANOATE INTERMEDIATE BY MEANS OF ONE-POT SYNTHESIS

机译:通过单盆合成制备Laninamivir octanoate中间体的方法

摘要

The present invention relates to the technical field of medicine synthesis, and specifically relates to a method for preparing a laninamivir octanoate intermediate by means of one-pot synthesis. The method for preparing a laninamivir octanoate intermediate by means of one-pot synthesis comprises: subjecting a compound as represented by formula (4) to a reaction in the presence of R1OH, NaH and (R1O)2CO to obtain a compound as represented by formula (5), wherein R1 is benzyl, substituted benzyl, or allyl. A laninamivir octanoate intermediate compound (5) is innovatively synthesized from a compound (4) by means of using one-pot synthesis; the reaction is gentle and rapid, and the next-step reaction can be carried out after simple post-treatment; energy consumption is saved, the pollution is reduced, operation is simple and the cost is low, such that the method is suitable for industrial production. The laninamivir octanoate intermediate compound (5) prepared by means of using one-pot synthesis has a yield of at least 87%.
机译:本发明涉及药物合成技术领域,并且具体涉及通过一种罐合成制备Laninamivir octanoate中间体的方法。通过单盆合成制备兰宁酰氨酸辛酸辛酸中间体的方法包括:使用式(4)表示的化合物对R 1 OH,NaH和(R 1 O)2CO存在的反应进行,得到如式所代表的化合物(5),其中R1是苄基,取代苄基或烯丙基。通过使用单罐合成,兰宁纳米啶酸辛酸中间体化合物(5)由化合物(4)创新地合成;反应温和,快速,并且可以在简单的后处理后进行下一步反应;能量消耗保存,污染降低,操作简单,成本低,使该方法适合工业生产。通过使用单罐合成制备的甘氨酸辛酸中间体化合物(5)的产率至少为87%。

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