Synthesis method of Avibactam intermediate
The invention discloses a synthesis method of an Avibactam intermediate, and belongs to the technical field of the medicine chemical synthesis. The synthesis method comprises the following steps: reacting pyroglutamate containing an amino protecting group with trimethylsulfoxonium iodide in a reacti...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a synthesis method of an Avibactam intermediate, and belongs to the technical field of the medicine chemical synthesis. The synthesis method comprises the following steps: reacting pyroglutamate containing an amino protecting group with trimethylsulfoxonium iodide in a reaction solvent under the effect of the carbonate to obtain the Avibactam intermediate. The problems thata strong alkali process method in the prior art is large in potential safety hazard, relatively difficult in process control and high in impurity content are avoided, and the synthesis method disclosed by the invention is mild in reaction condition, simple in operation, high in process operability security, high in yield, high in product purity and suitable for the industrial production.
本发明公开了种阿维巴坦中间体的合成方法,属于药物化学合成技术领域。本发明的合成方法将带有氨基保护基的焦谷氨酸酯与三甲基碘化亚砜在碳酸盐的作用下于反应溶剂中反应制得阿维巴坦中间体,避免了现有技术中的强碱工艺方法存在的安全隐患大、工艺控制较难、杂质多的问题,本发明的合成方法反应条件温和,操作简单,工艺操作安全性高,收率高、产品纯度高,适于工业化生产。 |
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