Cefmenoxime hydrochloride compound and synthesizing method thereof

A technology of cefmenoxime hydrochloride and a synthesis method, applied in the field of cefmenoxime hydrochloride compound and its synthesis, can solve the problems of low synthesis yield of cefmenoxime acid, high production cost, unsuitable for industrialized production and the like

Active Publication Date: 2012-10-17
ZHEJIANG JIANFENG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the technical defect that the synthesis yield of cefmenoxime hydrochloride is not high in the prior art, the production cost is high, and is not suitable for industrialized...

Method used

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  • Cefmenoxime hydrochloride compound and synthesizing method thereof
  • Cefmenoxime hydrochloride compound and synthesizing method thereof
  • Cefmenoxime hydrochloride compound and synthesizing method thereof

Examples

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Embodiment 1

[0070] The preparation of embodiment 1 cefmenoxime hydrochloride

[0071] This product is cefmenoxime hydrochloride, its structural formula is:

[0072]

[0073] Molecular formula: C 16 h 17 N 9 o 5 S 3 1 / 2HCl molecular weight: 529.79;

[0074] Physical and chemical properties: This product is white to light yellow crystal or crystalline powder, odorless, or slightly special odor, slightly bitter taste, hygroscopic.

[0075] This product is easily soluble in formamide, slightly soluble in methanol, very slightly soluble in water, insoluble in ethanol and ether; at 0.1mol / L

[0076] Soluble in phosphate buffer (pH6.8).

[0077] This product is a broad-spectrum semi-synthetic cephalosporin antibiotic, which achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell walls.

[0078] In vitro tests have shown that this product has effects on both Gram-positive and Gram-negative bacteria.

[0079] The preparation of cefmenoxime hydrochloride is descr...

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Abstract

The invention relates to the field of pharmacy, and especially related to a cefmenoxime hydrochloride compound and a synthesizing method thereof. The cefmenoxime hydrochloride compound has a formula shown below, and is prepared with a method comprising the steps that: (1) a cefoperazone precursor 7-ATCA.HCl and AE active ester are subjected to a condensation reaction under the existence of CH2Cl2and an alkalizing agent; and the obtained product is subjected to extraction, decolorization, press-filtration, neutralization, rejection filtration, and drying, such that cefmenoxime acid CMX-H is prepared; (2) the cefmenoxime acid is completely dissolved by using sodium carbonate; the obtained product is subjected to decolorization, press-filtration, neutralization, decolorization, filtration, crystallization, washing, and drying, such that a cefmenoxime hydrochloride half-finished product is prepared; a jet mill is started; and the material is crushed and is filled in aluminum bottles. According to the invention, cefmenoxime acid is prepared into crystals, such that the product purity is greatly improved, and the product quality is ensured. Also, the method provided by the invention is advantaged in small three-waste volume, simple preparation process, and low cost. Therefore, the method is suitable for the industrialized productions of our nation.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a cefmenoxime hydrochloride compound and a synthesis method thereof. Background technique [0002] Cefmenoxime hydrochloride is the third-generation cephalosporin antibiotic researched by Japan's Takeda Pharmaceutical Co., Ltd. in the 1970s. It was launched in Japan in 1983 under the trade name of Bestea, and then it was sold in Taiwan Province, China, and Taiwan respectively. France, Germany, Austria, South Korea, the United States, etc. are listed under different trade names, and their quality standards have been recorded in the 24th edition of the United States Pharmacopoeia and the Japanese Antibiotic Standards Explanation (1995 edition). [0003] Cefmenoxime hydrochloride is a third-generation cephalosporin, which has antibacterial effects on Gram-negative and positive aerobic and anaerobic bacteria. Among Gram-negative bacteria, the antibacterial effect on Escherichia coli and Kleb...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/06
Inventor 蒋晓萌黄金龙张春良沈泉郑昆武杜平洋
Owner ZHEJIANG JIANFENG PHARM CO LTD
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