Preparation method of 1-N-ethyl gentamicin Cla

A technology of ethyl gentamycin and ethyl gentamycin, which is applied in the field of preparation of medicinal raw materials, can solve the problems of low yield, avoid side reactions of alkylation, enhance polarization, and avoid hydrolysis Effect
CN101928311BActive Publication Date: 2012-09-05CHANGZHOU FANGYUAN PHARMA +1
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Patents(China)
Current Assignee / Owner
CHANGZHOU FANGYUAN PHARMA
Publication Date
2012-09-05

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Abstract

The invention discloses a preparation method of 1-N-ethyl gentamicin Cla, which comprises the following steps of: reacting 3,2',6'-tri-N-acetyl gentamicin Cla with hexamethyldisilazane in a trichloromethane solvent under the catalysis of concentrated sulfuric acid to generate 3,2',6'-tri-N-acetyl-5,2'',4''-tri(trimethylsilyl) gentamicin Cla; carrying out N-alkylation reaction on the 3,2',6'-tri-N-acetyl-5,2'',4''-tri(trimethylsilyl) gentamicin Cla and acetaldehyde in a dichloromethane solvent at a temperature of 8-12 DEG C; carrying out reduction reaction with potassium borohydride; then hydrolyzing with an NaOH solution to obtain hydrolyzate of the 1-N-ethyl gentamicin Cla; and post-processing the hydrolyzate to obtain a finished product of the 1-N-ethyl gentamicin Cla. The method has the advantage of higher yield of the1-N-ethyl gentamicin Cla.
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Description

Technical field

[0001] The invention relates to a preparation method of medicinal raw materials, in particular to a kind of 1-N-ethyl gentamicin C 1a The preparation method. Background technique

[0002] Chinese patent document CN1040177C (application number 93112412. 3) discloses a method containing 1-N-ethyl gentamicin C 1a Or its salt medicinal preparation and preparation method.

[0003] Among them is 3,2',6'-tris-N-acetyl gentamicin C 1a (β… ) Preparation of 1-N-ethyl gentamicin C 1a (β…€) The method is: directly use acetaldehyde to 3,2',6'-tri-N-acetyl gentamicin C 1a Carry out N-alkylation, then reduce with sodium borohydride aqueous solution to obtain 3,2',6'-tris-N-acetyl-1-N-ethylgentamycin C 1a , Then purified with YPR-β…‘ macroporous resin column, and then hydrolyzed with sodium hydroxide to obtain 1-N-ethyl gentamicin C 1a Hydrolyzed liquid, and finally after treatment to obtain 1-N-ethyl gentamicin C 1a (β…€) The finished product. The disadvantage of this method is: 3,2',6'-t...

Claims

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