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A kind of Tedizolid phosphate compound and preparation method thereof

A technology of tedizolid phosphate and its compound, which is applied in the field of tedizolid phosphate compound and its preparation, can solve the problems such as the need to improve the purity, many types of impurities, and high impurity content, and achieve the improvement of MRSA antibacterial activity, low water content, and stability Good results

Active Publication Date: 2017-11-28
SHANDONG LUOXIN PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN102177156A discloses a method for preparing oxazolidinones and a composition containing oxazolidinones. The yield of the method for purifying TR-701 is low, and the obtained TR-701 has many types of impurities (detected by the present invention as 8 species), the impurity content is high, especially the content of dimer impurities, the moisture content is also high, and the purity still needs to be improved
[0006] CN101982468B discloses oxazolidinone derivatives and pharmaceutical compositions containing the derivatives. Example 58 discloses the preparation method of tedizolid phosphate, and the prepared tedizolid phosphate has many types of impurities (detected by the present invention as 19 kinds ), the impurity content is high, especially the content of dimer impurities, the moisture content is also high, and the purity still needs to be improved
[0007] CN102439006A provides a crystal form of TR-701FA and its preparation method. This method avoids more toxic solvents, is more stable, and is not easy to absorb moisture, and reduces the amount of dimer impurities. However, the disclosed TR-701FA crystal form The preparation method yield is low, and impurity kind is many (detected as 18 kinds by the present invention), and impurity content is high, especially dimer content is still higher, and purity needs to be improved
[0008] CN104327119A provides a preparation method of tedizolid phosphate, the obtained tedizolid phosphate still has many types of impurities (18 kinds detected by the present invention), and the content of impurities is high, especially the content of dimer impurities is relatively high , the moisture content is also high, and the purity still needs to be improved

Method used

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  • A kind of Tedizolid phosphate compound and preparation method thereof
  • A kind of Tedizolid phosphate compound and preparation method thereof
  • A kind of Tedizolid phosphate compound and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0089] The preparation method of embodiment 1 tedizolid phosphate compound

[0090] 1) Add the tedizolid phosphate crude product prepared by the method in Example 7 of CN102177156A into a mixed solvent of water and methanol, add while stirring, the stirring speed is 360 rpm, and the adding speed is 50 ml / min, and the mixed solvent The volume mass ratio with tedizolid phosphate crude product is 30ml:1g, and the volume ratio of water and methanol is 1:2;

[0091] 2) After heating and refluxing to dissolve the clear, filter through a 0.45 μm microporous membrane, drop the temperature to room temperature within 1.5 hours, and keep at room temperature for 3 hours;

[0092] 3) Further cool down to -3.5°C at a rate of 5°C / h, let stand for 3.5 hours, filter with suction, wash the filter cake with a mixed solvent of water and methanol, the volume ratio of water and methanol is 1:2;

[0093] 4) Vacuum drying at a temperature of 45° C. to obtain tedizolid phosphate compound.

[0094] T...

Embodiment 6

[0097] The HPLC detection data of Example 6 are shown in Table 3.

Embodiment 11

[0098] The HPLC detection data of Example 11 are shown in Table 4.

[0099]

[0100]

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PUM

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Abstract

The invention relates to a tedizolid phosphate compound, which contains a trace amount of pyrophosphate, the content of the tedizolid phosphate is ≥98%, and the content of the pyrophosphate is ≤0.2%. The present invention also relates to the preparation method of the tedizolid phosphate compound. The tedizolid phosphate compound provided by the present invention has few types of impurities and low content, especially the dimer content is greatly reduced, the moisture content is small, and the stability is good. Surprisingly, the test found that compared with the prior art, the bioavailability of the compound was significantly improved, and the curative effect and adverse reactions were superior to the prior art, especially the antibacterial activity against MRSA was significantly improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tedizolid phosphate compound and a preparation method thereof. Background technique [0002] The treatment of infectious diseases such as skin and soft tissue infections (SSSIs), pneumonia, sepsis, and endocarditis caused by Gram-positive bacteria is still facing severe challenges in today's advanced modern medicine. Taking methicillin-resistant Staphylococcus aureus (MRSA) as an example, MRSA appeared 2 years after the clinical application of methicillin, and after more than 50 years, the bacteria has been widely spread in hospitals all over the world. Since the early 1990s, community-acquired MRSA (CA-MRSA) appeared and spread globally, changing the old idea that MRSA infection only occurs in hospital settings. The problem of drug resistance in Gram-positive bacteria is not limited to MRSA, including challenges posed by vancomycin-resistant enterococci (VRE), ma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6558
Inventor 王亚飞龚红银王华
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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