Preparation method of avibactam intermediate

The invention relates to the technical field of drug synthesis, discloses a preparation method of an avibactam intermediate, and solves the technical problems that purification is complicated, and a reagent is not environment-friendly or is not suitable for large-scale production in the prior art. T...

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Hauptverfasser: LI YINLAN, CHEN YONG, ZHAO YULING, YANG QIMING, DAI ZHIDONG, ZHOU CUILIAN, XIAO MAOLING, GUO RUI, HUANG JINYU
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the technical field of drug synthesis, discloses a preparation method of an avibactam intermediate, and solves the technical problems that purification is complicated, and a reagent is not environment-friendly or is not suitable for large-scale production in the prior art. The yield of the process from the (2S, 5R)-5-((benzyloxy) amino) piperidine-2-carboxylic acid ethyl ester to the (2S, 5R)-6-(benzyloxy)-7-oxo-1, 6-diazabicyclo [3.2. 1] octane-2-formamide reaches 87%, the purification process of the process from the (2S, 5R)-6-(benzyloxy)-7-oxo-1, 6-diazabicyclo [3.2. 1] octane-2-formamide to the avibactam sodium salt is simple, the reaction conditions are mild, the method is environmentally friendly, and the method is suitable for industrial production. And large-scale industrial production can be realized. 本发明涉及药物合成技术领域,公开了一种阿维巴坦中间体的制备方法,解决现有技术中的纯化复杂,试剂对环境不友好或者不适合大规模生产的技术问题。本发明(2S,5R)-5-((苄氧基)氨基)哌啶-2-羧酸乙酯到(2S,5R)-6-(苄氧基)-7-氧代-1,6-二氮杂双环[3.2.1]辛烷-2-甲酰胺的过程收率高达87%,(2S,5R)-6-(苄氧基)-7-氧代