A kind of preparation method of 4-acetoxy-2-azetidinone compound

An azetidinone, acetoxy technology, applied in directions such as organic chemistry, can solve problems such as unfavorable large-scale production, high price, harsh reaction conditions, etc., achieve convenient recovery and reuse, reduce production costs, and be easy to separate. The effect of purification
CN103539813BInactive Publication Date: 2016-05-04TAIZHOU VOCATIONAL & TECHN COLLEGE +1
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Patent Information

Authority / Receiving Office
CN ¡ China
Patent Type
Patents(China)
Current Assignee / Owner
TAIZHOU VOCATIONAL & TECHN COLLEGE
Publication Date
2016-05-04
Estimated Expiration
Not applicable ¡ inactive patent

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Abstract

The invention relates to a preparation method of 4-acetyloxy-2-azetidinone compounds, and is used for solving the problem that the large-scale industrial production cannot be favorably realized because of defects such as severe reaction condition, complex treatment process, high cost, serious environment pollution and the like in the prior art. The method provided by the invention comprises the step of carrying out oxidization deacidification in the existence of a dehydrating agent N, N'-dicyclohexylcarbodiimide and an oxidizing agent peroxyacetic acid by taking 4-carboxyl-2-azetidinone compounds I as raw materials to obtain the 4-acetyloxy-2-azetidinone compounds II. A heavy metal oxidizing agent or catalyst is prevented from being used in the oxidization deacidification process, so that the residue and discharge of heavy metals and environmental pollution caused by the heavy metals are greatly reduced. Byproducts generated in a reaction process can be conveniently recycled, so that the production cost is reduced to the great extent, and the preparation method is more excellent on the aspect of economical efficiency. The method is mild in reaction condition, simple and convenient to operate and suitable for large-scale production; the 4-acetyloxy-2-azetidinone compounds are easy to separate and purify and high in yield.
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Description

technical field

[0001] The invention belongs to the technical field of organic synthesis and chemical medicine preparation, and relates to a method for preparing 4-acetoxy-2-azetidinone compounds, in particular to a method for preparing penem drug intermediates 4-acetyl The preparation method of oxy-2-azetidinone compound. technical background

[0002] The 4-acetoxy-2-azetidinone compound represented by formula II is an important intermediate for the synthesis of penem drugs. Penem drugs are a new group of β-lactam antibiotics, which have the broadest antibacterial spectrum and the strongest antibacterial effect among the antibacterial drugs developed so far. Since the discovery of thiamycin in 1976, the research on penem drugs has made great progress. So far, the penems that have been marketed in the world mainly include imipenem, panipenem, and the United States. Luo Penem (Meropenem), there are many varieties in clinical trials. Therefore, it is of great significance t...

Claims

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