Linezolid crystal form VI and preparation method thereof

A technology of linezolid and its crystal form, which is applied in the field of linezolid crystal form VI and its preparation, can solve the problems of high power consumption, large consumption of organic solvents for crystal form A, easily damaged product purity, etc., and achieves mild process conditions, Guarantee the ideal effect of medication effect and dissolution effect

Active Publication Date: 2014-09-10
CHENGDU XINJIE HIGH TECH DEV CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The preparation of crystal form A needs to consume a large amount of organic solvents, and the process conditions are strictly controlled; crystal forms III and IV need to be prepared under high temperature conditions, which consumes a lot of power and easily destroys the purity of the product
Moreover, the dissolution rate (dissolution effect) of the existing linezolid crystal forms is not particularly ideal, and the drug effect cannot be effectively guaranteed

Method used

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  • Linezolid crystal form VI and preparation method thereof
  • Linezolid crystal form VI and preparation method thereof
  • Linezolid crystal form VI and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 5g of linezolid crystal form A (form A disclosed in WO 2011 / 050826), add it to 75ml of water, cool down to 0°C, add 2mol / L concentrated hydrochloric acid, stir until the solid dissolves completely, and keep the internal temperature (that is, keep Solution temperature) is 0°C, dropwise add potassium hydroxide aqueous solution with a mass percentage concentration of 20%, adjust PH=7, continue to heat and stir for 30 minutes, filter, wash the solid with water until neutral, and dry Delineate under reduced pressure at 40°C Azolamide crystal form VI 4.81g.

[0027] The crystal form VI of linezolid obtained in this example, the X-ray powder diffraction pattern of linezolid crystal form VI is as follows: figure 1 (The abscissa is the 2-theta angle (°), the ordinate is the relative intensity (%), and the number marked in the figure is the interplanar distance (?)). The X-ray powder diffraction pattern data are shown in the following table:

[0028] Relative Stre...

Embodiment 2

[0031] Weigh 5g of linezolid crystal form II (form II disclosed in EP1255754), add it to 25ml of water, add 3mol / L formic acid, stir until the solid dissolves completely, keep the internal temperature at 5°C, and dropwise add 32% (mass %) sodium hydroxide aqueous solution, adjust PH=12, continue to stir for 30 minutes, filter, wash the solid with water until neutral, and dry under reduced pressure at 50°C to obtain 4.77g of linezolid crystalline form VI.

Embodiment 3

[0033] Weigh 5g of linezolid crystal form III (form III disclosed in EP2100884), add it to 40ml of water, add acetic acid, stir until the solid dissolves completely, add 50% potassium carbonate aqueous solution to it dropwise at room temperature, adjust the pH=10, continue Stir for 30 minutes, filter, wash the solid with water until neutral, and dry under reduced pressure at 40°C to obtain 4.72 g of Linezolid Form VI.

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Abstract

The invention relates to a linezolid crystal form VI and a preparation method thereof. In the X-ray powder diffraction spectrum, the crystal form VI powder has absorption peaks at the diffraction angle 2-theta=11.25, 16.27, 16.70, 18.95, 19.69, 22.73, 25.09, 25.31, 26.22, 26.55, 27.54 and 29.60, wherein the error range of the angle 2-theta is + / -0.1. The linezolid crystal form VI provided by the invention has favorable dissolution rate and ideal dissolution effect, and can ensure the medicinal effect; and by using water as the solvent, the preparation method of the crystal form has the advantages of mild technical conditions, no organic solvent to be recycled or discharged, environmental protection and energy saving.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a linezolid crystal form VI and a preparation method thereof. Background technique [0002] Linezolid, the chemical name is (S)-N[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methanol Base] Acetamide, the first oxazolidinone antibacterial drug developed by Pfizer in the United States, is used for the treatment of bacteremia caused by vancomycin enterococcus (VRE), methicillin-resistant Staphylococcus aureus (MRSA) Pneumonia and generalized skin infections and bacteremia caused by penicillin-resistant Streptococcus pneumoniae (PRSP). Its structural formula is: [0003] . [0004] WO 2011 / 050826 discloses crystal form A and its preparation method. The powder diffraction of this crystal form has characteristic diffraction angle (2θ) peaks: 7.6, 9.6, 13.6, 14.9 18.2 18.9, 21.2, 22.3, 25.6, 26.9, 27.9, 29.9; Chinese patent ZL 01803448.9 discloses its Ⅱ crystal f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D263/20
Inventor 叶丁高建刘力超蒲洪欧世荣王晓玲唐雪枫
Owner CHENGDU XINJIE HIGH TECH DEV CO LTD
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