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Preparation method of isepamicin sulfate (I)

A technology of isopamicin sulfate and ethyl acetate, which is applied to the preparation of sugar derivatives, chemical instruments and methods, sugar derivatives, etc., can solve the problems of low yield, long production cycle, and low product purity, and achieve High product purity and yield, low synthesis cost, and the effect of synthesis period

Inactive Publication Date: 2016-01-20
WUXI FORTUNE PHARMA
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Problems solved by technology

[0006] However, the above preparation method has the disadvantages of high synthetic route cost, long production cycle, low product purity and low yield, so it is not suitable for industrialized mass production

Method used

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  • Preparation method of isepamicin sulfate (I)
  • Preparation method of isepamicin sulfate (I)
  • Preparation method of isepamicin sulfate (I)

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Embodiment Construction

[0023] The present invention will be described in detail below in conjunction with various embodiments, but it should be noted that these embodiments are not limitations of the present invention, and those of ordinary skill in the art can make functional, method, or structural equivalent transformations or replacements based on these embodiments. , all fall within the protection scope of the present invention. Unless otherwise specified in the description, the components and raw materials in each example of the present invention are of analytical grade.

[0024] In addition, "g" in each embodiment is the weight unit "gram"; "h" is the time unit "hour"; "ml" is the volume unit "milliliter"; "room temperature" is 23°C; Liquid Chromatographic Detection".

[0025] Step 1): Use gentamicin B (II) as the starting material, protect with the reaction reagent and trimethylsilylethoxycarbonyl chloride to obtain the intermediate (III), and the details are as follows.

[0026] In a 250ml...

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Abstract

The invention discloses a preparation method of isepamicin sulfate (I). The method comprises the following steps that (1) gentamicin gentamycin B (II) serves as a starting raw material, and after a reaction reagent and trimethyl silicone ethoxy carbonyl chloride protect, an intermediate (III) is obtained; (2) the intermediate (III) reacts with N,N-dicyclohexylamine and is coupled with N-phthalic anhydride-(S)-isoserine, and the product is subjected to column chromatography isolation to obtain an intermediate (IV); (3) the intermediate (IV) is de-protected and acidified by vitriol to obtain a crude product, and the crude product is re-crystallized with anhydrous alcohol to obtain isepamicin sulfate (I). The preparation method of the isepamicin sulfate (I) disclosed by the invention has the advantages of low synthesizing cost, short synthesizing period, and high product purity and yield, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a preparation method of the aminoglycoside antibiotic isepamicin sulfate (I). Background technique [0002] Isepamicin sulfate (Ⅰ) is an aminoglycoside antibiotic, mainly used for Escherichia coli, Citrobacter, Klebsiella, Enterobacter, which are sensitive to it (including gentamicin resistance) Genus Serratia, Morganella morganii and Pseudomonas aeruginosa cause various infectious diseases, mainly bacterial pneumonia, pyelonephritis, cystitis, peritonitis, etc., and are widely used clinically. [0003] At present, the preparation method of Isepamicin Sulfate (I) mainly contains following several kinds: [0004] U.S. patent application US5442047A discloses a preparation method of isopamicin sulfate, which uses gentamicin B as a starting material, first reacts with a metal chelator, and then uses 2-formylmercaptobenzothiazole to selectively protect The 3,6'-amino group of genta...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/236C07H1/00
Inventor 徐建国王彬彬王庆林王涛付静史佳栋张莹
Owner WUXI FORTUNE PHARMA
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