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Secnidazole water-soluble salt and preparation method thereof

A technology of secnidazole phosphate and secnidazole, which is applied in the field of modified chemicals and their modification, and can solve the problems of inconvenient production, storage and transportation, long time, large amount of solvent and the like

Inactive Publication Date: 2008-09-03
HEFEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, when secnidazole is instilled, the amount of solvent is large and the time is long, which causes unnecessary pain to the patient.
In addition, the large amount of solvent also brings inconvenience to the production and storage process.
[0004] U.S. Patent No. 5,574,167 prepared a series of benzoate and fatty acid esters of secnidazole for the purpose of improving stability and improving adverse reactions, but failed to improve the water solubility of secnidazole

Method used

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  • Secnidazole water-soluble salt and preparation method thereof
  • Secnidazole water-soluble salt and preparation method thereof
  • Secnidazole water-soluble salt and preparation method thereof

Examples

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Comparison scheme
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Embodiment 1

[0027] The preparation of embodiment 1 secnidazole phosphate disodium salt

[0028] Dissolve 4.6g of phosphorus oxychloride in 60mL of DMC at room temperature, put it into a three-necked flask, add 5.5g of secnidazole several times under stirring, stir for 2 hours after the addition, and precipitate a large amount of off-white solid. Raise the temperature to reflux and stir the reaction for more than 10 hours until no more acid gas is released. The liquid was poured out and distilled to dryness under reduced pressure to obtain a red solid residue. 25mL of water was added under stirring, and stirred at 50°C for 1h for hydrolysis. Activated carbon decolorizes and filters, and concentrates to dryness under reduced pressure below 60°C to obtain a reddish-brown clear transparent oil (solid after cooling), which mainly contains secnidazole phosphate. Add an appropriate amount of 90% methanol to fully dissolve, add a slight excess of sodium carbonate several times in a 40°C water b...

Embodiment 2

[0030] The preparation of embodiment 2 secnidazole dipotassium phosphate

[0031] The same operation as in Example 1, but sodium carbonate was changed to potassium carbonate, and the product was vacuum-dried at 160° C., and 5.5 g of secnidazole was added to obtain 5.6 g of anhydrous secnidazole dipotassium phosphate.

Embodiment 3

[0032] Embodiment 3 secnidazole succinic acid monoester

[0033] Cyclohexane 50ml, succinic anhydride 2.5g and pyridine 0.1mL, mix well and heat to 70°C; add 4.625g secnidazole. Reflux for more than 18 hours. Cool the reaction solution to room temperature, thick solids precipitate out at the bottom of the flask, pour out the upper liquid, add an appropriate amount of ether / carbon disulfide (4:1) to the flask, heat and stir to precipitate solids, filter, and dry to obtain secnidazole amber Acid monoester 5.2g, melting point 103-105°C. The solid is soluble in water and ethanol.

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Abstract

The invention relates to a soluble derivate of secnidazole for curing amebic dysentery, that is secnidazole microcosmic salt or sufosuccinate monoester, wherein the compounds with above structure are chemical derivates of secnidazole which can act in the range of secnidazole. The aqueous solubility of the derivates is substantially better than secnidazole, so can be prepared to be a new type that the secnidazole can not, such as sterile powder for injecting. The invention further relates to preparation methods for secnidazole microcosmic salt or sufosuccinate monoester.

Description

1. Technical field [0001] The invention relates to a modified chemical drug and a modification method thereof, in particular to a water-soluble secnidazole salt and a preparation method thereof. 2. Background technology: [0002] Amoeba and protozoa have seriously affected human health. There are as many as 500 million people in the world carrying amoeba histolytica, about 250 million people infected with Giardia, and more than 200 million people infected with Trichomonas. Secnidazole is very effective in the treatment of the above infections. Secnidazole, chemical name: 1-(2-hydroxypropyl)-2-methyl-5-nitroimidazole. It has been reported that a single dose of secnidazole 2g (or 30mg / Kg) is administered, and it is very effective for the treatment of giardiasis, acute intestinal amoebiasis and vaginal trichomoniasis. Cysts and hepatic amoebas are also inhibitory. Single-dose administration not only means great convenience for patients, but the resulting relief of drug press...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6506C07D233/94A61P33/02
Inventor 姚日生邹国勇邓胜松朱慧霞何红波
Owner HEFEI UNIV OF TECH
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