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Nitroimidazole derivative for treatment

A kind of morpholinidazole phosphate, application technology, applied in the field of nitroimidazole derivatives, can solve problems such as poor water solubility

Active Publication Date: 2006-08-02
江苏国丹生物制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Morpholinidazole is also undergoing clinical trials, but this type of compound has poor water solubility, and compound agents must be used to achieve satisfactory water-soluble preparations, such as intravenous preparations

Method used

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  • Nitroimidazole derivative for treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: the preparation of morpholinidazole phosphate

[0016] Mix 22g of ornidazole, 30g of sodium iodide, and 400ml of acetonitrile, stir and heat to reflux, keep warm for 30 minutes, cool to room temperature, then add 13g of 4-hydroxypiperidine and 20g of triethylamine, stir and heat to reflux, keep warm for reaction After 5 hours, the reaction was completed, acetonitrile was recovered, 150ml of distilled water was added, heated until completely dissolved, filtered while hot, allowed to cool, filtered, washed with water, and dried to obtain 20.3g of an off-white solid, namely intermediate 1.

[0017] Put 140g of the intermediate in 300ml of acetonitrile, under stirring, add 40ml of phosphorus oxychloride dropwise, control the reaction temperature at 10-15°C, after the dropwise addition, continue to keep warm for 1 hour, cool and crystallize for 5h (0°C), filter, The filter cake was dissolved in 200ml of water, hydrolyzed for 40min, distilled under reduced press...

Embodiment 2

[0018] Embodiment 2: the preparation of L-morpholinidazole phosphate

[0019] Levomorphinidazole phosphate was prepared according to the preparation method of Example 1, except that ornidazole was replaced by levomorphinidazole (ee value 0.99).

Embodiment 3

[0020] Embodiment 3: the preparation of dexmorphonidazole phosphate

[0021] Levomorphinidazole phosphate was prepared according to the preparation method of Example 1, except that ornidazole was replaced with D-ornidazole (ee value 0.99).

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PUM

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Abstract

The present invention relates to disease treating nitroimidazole derivative, and the compound may be used in preparing medicine for resisting anaerobic bacteria and trichomonas.

Description

technical field [0001] The invention relates to a nitroimidazole derivative used for treatment, and the compound can be used for preparing medicines against anaerobic bacteria and trichomonas. technical background [0002] Nitroimidazole antibacterial drugs are powerful anti-anaerobic bacteria and anti-protozoal drugs. At present, there are mainly metronidazole, tinidazole, secnidazole and ornidazole on the market. Morpholinidazole is also being studied in clinical trials, but these compounds are poorly water-soluble, and complex agents must be used to achieve satisfactory water-soluble preparations, such as intravenous preparations. However, it is always desirable to reduce the number of ingredients in the formulation in order to reduce possible side effects in the patient. Contents of the invention [0003] The object of the present invention is to provide a kind of morpholinidazole phosphate with good water solubility, pH value of aqueous solution acidity close to pH v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6533A61K31/675A61P31/04
Inventor 苏红军许红宝
Owner 江苏国丹生物制药股份有限公司
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