6-APA (6-amino-penicillanic acid) and preparation method thereof

A technology of aminopenicillic acid and potassium penicillin, applied in the field of penicillin, can solve the problems of high investment, high cost, large amount of organic solvent and the like

Inactive Publication Date: 2016-11-09
FARMASINO PHARMA ANHUI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the enzymatic cleavage method of solid penicillin potassium salt is generally used in the production of 6-APA in the world. This method is mature, but the yield is low and the cost is high. At the same time, the amount of organic solvent used is large, and the investment in environmental protection is large.

Method used

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  • 6-APA (6-amino-penicillanic acid) and preparation method thereof
  • 6-APA (6-amino-penicillanic acid) and preparation method thereof
  • 6-APA (6-amino-penicillanic acid) and preparation method thereof

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preparation example Construction

[0036] image 3 It is a flow chart of the preparation process according to an embodiment of the present invention. see image 3 , The present invention directly adopts the potassium carbonate back-extraction liquid of penicillin potassium to carry out the process of enzymatic cleavage to prepare 6-APA. Catalytic cracking is the result of the joint action of carbocation reaction mechanism and free radical reaction mechanism. With enzyme-catalyzed cleavage, enzymes either speed up or slow down the action of chemical reactions. The invention uses enzymes to promote catalytic cracking, so that carbocations of penicillin potassium soaked in the potassium carbonate stripping liquid participate in the reaction, and the reaction speed can be accelerated to a certain extent.

[0037] Penicillin Potassium, also known as Bian Penicillin, is a white crystalline powder, odorless or slightly specific odor, hygroscopic. Penicillin Potassium is easily soluble in water, normal saline, and ...

Embodiment 1

[0070] Raw material ratio:

[0071] Potassium penicillin was used and soaked in potassium carbonate stripping solution. Penicillin Potassium, also known as Bian Penicillin, is a white crystalline powder, odorless or slightly specific odor, hygroscopic.

[0072] According to an embodiment of the present invention, the raw materials can be weighed precisely, and "precisely weighed" means that the weighed weight should be accurate to one thousandth of the weighed weight. "Precise measurement" means that the accuracy of the measured volume should meet the accuracy requirements of the volume pipette in the national standard.

[0073] The present invention directly adopts the potassium carbonate back-extraction solution of penicillin potassium to carry out enzymatic cleavage reaction to prepare 6-APA. The carbocation of penicillin potassium participates in the reaction, which can speed up the reaction to a certain extent. Penicillinase cleavage can be catalyzed by immobilized enz...

Embodiment 2

[0080] According to another embodiment of the present invention, 6-APA having the molecular structure shown below is produced

[0081]

[0082] 6-APA can introduce different side chains to obtain various penicillins with different drug effects.

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Abstract

The invention provides a preparation method of 6-APA (6-amino-penicillanic acid). 6-APA is prepared from a potassium carbonate reversed-extraction liquid of benzylpenicillin potassium directly, a molecular formula of 6-APA is C8H12N2O3S, and the molecular weight is 216.26. With the adoption of the process, a crystallization step can be omitted, and crystallization yield loss is avoided; extracting and washing processes of a penicillin solvent are optimized in a technical process; with the adoption of the advanced preparation process, the preparation method is higher in yield and lower in cost.

Description

technical field [0001] The present invention relates to a kind of penicillin, especially a kind of 6-aminopenicillanic acid adopting advanced technology and its preparation method and application. Background technique [0002] Amoxicillin is one of the most commonly used penicillin-like broad-spectrum β-lactam antibiotics. It is a white powder with a half-life of about 61.3 minutes. It has a bacteriolytic effect and is mainly used to treat bacterial infections caused by susceptible microorganisms. Stable under acidic conditions, the gastrointestinal absorption rate reaches 90%. Amoxicillin has a strong bactericidal effect and a strong ability to penetrate cell walls. It is one of the most widely used oral penicillins at present, and its preparations include capsules, tablets, granules, dispersible tablets and so on. [0003] 6-aminopenicillanic acid (6-APA) is an important intermediate in the production of amoxicillin. 6-aminopenicillanic acid (6-APA) is also known as pe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P37/06C07D499/42
CPCC12P37/06C07D499/42
Inventor 燕立兵燕立波张明鹤杨生晋
Owner FARMASINO PHARMA ANHUI
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