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Ammonia maleate rubicin salt, and its preparing method and use

A kind of technology of amrubicin and amrubicin, which is applied in the field of amrubicin maleate and its preparation and use, and can solve the problems such as stability of amrubicin hydrochloride that is not disclosed

Inactive Publication Date: 2006-08-09
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of amrubicin hydrochloride itself as a drug or bulk drug is not disclosed

Method used

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  • Ammonia maleate rubicin salt, and its preparing method and use
  • Ammonia maleate rubicin salt, and its preparing method and use
  • Ammonia maleate rubicin salt, and its preparing method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: the preparation of amrubicin maleate salt freeze-dried powder

[0025] In a 250ml reaction bottle, put 4.84g (10.0mmol) of amrubicin (10.0mmol) and 1.16g (10.0mmol) of maleic acid, add 320ml of deionized water, stir and dissolve, filter with a microporous membrane, freeze-dry, and obtain lyophilized Powder 5.89g, yield 98.2%.

Embodiment 2

[0026] Embodiment 2: the preparation of amrubicin maleate salt

[0027] In a 2000ml reaction bottle, put 4.84g (10.0mmol) of amrubicin (10.0mmol) and 1.22g (10.5mmol) of maleic acid into it, add 420ml of methanol, stir and dissolve, filter, concentrate under reduced pressure at room temperature until turbid and crystals are precipitated, stir and drop After adding 240ml of isopropyl ether, a large number of orange-red crystals were gradually precipitated, then stirred at room temperature for 1 hour, filtered, washed with isopropyl ether, and vacuum-dried at room temperature to obtain 5.8 g of orange-red crystals, with a yield of 96.7%. Melting point: 146.9-147.8°C. X-diffraction pattern see figure 1 .

Embodiment 3

[0028] Embodiment 3: the preparation of amrubicin maleate salt

[0029] In a 2000ml reaction bottle, put 4.84g (10.0mmol) of amrubicin (10.0mmol) into it, 1.22g (10.5mmol) of maleic acid, add 420ml of methanol, stir and dissolve, concentrate under reduced pressure at room temperature until it becomes turbid and there are crystals, continue to concentrate until there is a large amount of Crystals were precipitated, then stirred at room temperature for 1 hour, filtered, washed with a small amount of methanol, and dried in vacuo at room temperature to obtain 4.48 g of orange crystals with a yield of 74.7%. Melting point: 145.7-146.8°C. The X-diffraction pattern is identical to the product of Example 1.

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Abstract

The invention relates to maleic acid ammonia pirarubicin salt and its preparation method, and its application in antineoplastics and pharmaceutical preparation. The preparation method includes reaction in solvent, freeze drying, or crystallizing.

Description

technical field [0001] The invention relates to amrubicin maleate and a preparation method thereof, a pharmaceutical composition containing the compound, and an application of the compound in preparing antitumor drugs and pharmaceutical preparations. Background technique [0002] Japanese patent JP3-5397 B2 and US patent 4,673,668 disclose the preparation of amrubicin hydrochloride and its use as a drug for cancer chemotherapy. Among them, amrubicin, the target compound specifically synthesized in the examples, was included, and amrubicin hydrochloride was prepared according to conventional methods. [0003] US Patent No. 6,376,469 also discloses the preparation of crystalline amrubicin hydrochloride with a stable crystal form. [0004] PCT document WO 9928331 A2 discloses a method for preparing amrubicin hydrochloride crystals by adding hydrochloric acid to a solution of amrubicin and adjusting the pH value. [0005] Japanese Patent No. JP 1-40493 A and US Patent No. 4,95...

Claims

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Application Information

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IPC IPC(8): C07H15/252A61K31/704A61K9/19A61P35/00
Inventor 钟慧娟吕爱锋
Owner JIANGSU HANSOH PHARMA CO LTD
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