Preparation method of nifuratel with high purity

A technology for nifuratel and crude nifuratel, which is applied in the field of preparation of nifuratel, can solve the problems of low reaction yield and achieve the effect of high purity and good appearance

Inactive Publication Date: 2010-03-24
BEIJING D VENTUREPHARM TECH DEV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The synthetic key intermediate of existing literature is consistent, only the method for obtaining key intermediate 3-amino-5-[methylthio) methyl]-2-oxazolidinone has proposed an improved method in front, and by 3-amino -5-[methylthio)methyl]-2-oxazolidinone and 5-nitrofurfural have the same method for synthesizing the final product, and the common feature of this step reaction is that the reaction yield is low

Method used

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  • Preparation method of nifuratel with high purity
  • Preparation method of nifuratel with high purity
  • Preparation method of nifuratel with high purity

Examples

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Embodiment 1

[0026] Preparation of 5-nitrofurfural

[0027] Into a 20L reactor, add 7.15kg of isopropanol, 2.20kg of 5-nitrofurfural diethyl ester, 4.97kg of dilute nitric acid (mixed solution of 0.77kg of concentrated nitric acid and 4.20kg of distilled water), and heat to reflux for 2h. After cooling down to room temperature, the solution was kept for later use, and it was directly used in the next reaction.

Embodiment 2

[0029] Preparation of 5-nitrofurfural

[0030] In a 20L reactor, add 7.15kg of ethanol, 2.20kg of 5-nitrofurfural diethyl ester, 4.97kg of dilute sulfuric acid (mixed solution of 0.77kg of concentrated sulfuric acid and 4.20kg of distilled water), and heat to reflux for 2h. After cooling down to room temperature, the solution was kept for later use, and it was directly used in the next reaction.

Embodiment 3

[0032] Preparation of 5-nitrofurfural

[0033] In a 20L reactor, add 7.15kg of ethanol, 2.20kg of 5-nitrofurfural diethyl ester, 4.97kg of dilute nitric acid (mixed solution of 0.77kg of concentrated nitric acid and 4.20kg of distilled water), and heat to reflux for 2h. After cooling down to room temperature, the solution was kept for later use, and it was directly used in the next reaction.

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Abstract

The invention discloses a preparation process of nifuratel, which is suitable for industrialization, and a purifying method, including: taking 3-ammo-5-[(methylthio)methyl]-2-oxadixyl and 5-nitrofurfuraldiacetate as the initial raw materials, acid-hydrolyzing and docking to generate nifuratel, post-processing and recrystallizating to obtain a highly finished product. The highly finished product obtained by the method has high purity, the operating method is simple, the production cost is low, the yield is high, the preparation process is more suitable for industrialization, and the preparationprocess has the competition in the same processes.

Description

Technical field [0001] The invention relates to a method for preparing high-purity nifuratel. Background technique [0002] Nifuratel (Nifuratel) is 5-[(Methylthio)methyl]-3-[[(5-nitro-2-furanyl)methylene]amino]-2-oxazolidinone, (5-[(methylthio)methyl ]-3-[(5-Nitroglycylidene)amino]-2-oxazolidinone) has the following structure: [0003] [0004] Nifuratel is a drug developed by Monsanto Intalians S.P.A in Italy. It is a nitrofuran antibiotic drug and a broad-spectrum bactericide. It has a significant therapeutic effect on various vaginitis caused by bacterial, protozoan and fungal infections that cause women’s reproductive system infections. Its trichomonal activity is comparable to metronidazole. Equivalent, has antibacterial (G+, G+) effects, can effectively kill trachoma cells and mycoplasma, and has certain activity against Candida. Nifuratel and its topical preparations in the treatment of vaginal infections in women have a wide antibacterial spectrum, easy to take, short c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/12A61P31/04A61P15/02
Inventor 陈拥军谌伦华焦育红
Owner BEIJING D VENTUREPHARM TECH DEV
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