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
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creator LI YINLAN
CHEN YONG
ZHAO YULING
YANG QIMING
DAI ZHIDONG
ZHOU CUILIAN
XIAO MAOLING
GUO RUI
HUANG JINYU
description 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
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Preparation method of avibactam intermediate
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