Method for synthesizing avibactam intermediate compound

A synthesis method and compound technology, which can be used in organic chemistry, bulk chemical production, etc., can solve the problems of expensive raw materials, unfriendly environment, expensive process conditions, etc., and achieve the effect of mild reaction conditions, no heavy metal pollution, and environmental friendliness.
CN110437137APending Publication Date: 2019-11-12CHENGDU CLIMB PHARMA TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CHENGDU CLIMB PHARMA TECH
Publication Date
2019-11-12

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Abstract

The invention relates to a method for synthesizing an avibactam intermediate compound. The specific synthetic route of the method is as described in the specification. According to a technical schemeof the invention, no precious metal catalyst is used, and no heavy metal pollution is produced; high yield and low cost are realized; and the method is mild in reaction condition and friendly to environment, and can realize industrial production.
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Description

technical field

[0001] The invention belongs to the field of medicine preparation, and in particular relates to a synthesis method of an avibactam intermediate compound. Background technique

[0002] Avibactam is a novel β-lactamase inhibitor that can reversibly bind to the enzyme covalently. As a new type of enzyme inhibitor, avibactam has significant and extensive enzyme inhibitory effects, can restore or enhance the activity of combined antibiotics, and is of great significance to the treatment of clinical bacterial infections, especially drug-resistant bacterial infections.

[0003] Compound E1 is a key intermediate for the synthesis of avibactam, and its structural formula is:

[0004]

[0005] The synthetic method for preparing E1 in the prior art has more or less defects. For example, the synthetic route described in the patent document WO2013149136 is:

[0006]

[0007] This route requires the use of metal iridium [Ir(COD)Cl] 2 catalysts resulting in high cos...

Claims

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