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Disodium tedizolid phosphate and preparation method thereof

A technology of tedizolid phosphate disodium salt and tedizolid phosphate, applied in the field of medicine, can solve the problems of unfavorable freeze-dried powder injection preparation, affecting preparation quality, poor hygroscopic stability of disodium salt, etc., and achieving excellent stability , The effect of low hygroscopicity and small types of organic solvents

Active Publication Date: 2015-04-22
石药集团中诺药业(石家庄)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Freeze-dry the disodium salt solution to prepare sterile freeze-dried powder for injection. The disodium salt is easy to dissolve, which is conducive to redissolving in sterile water to obtain a solution, which can be directly added to the intravenous infusion bag, which can contain isotonic solution Such as 0.9% sodium chloride solution or 5% glucose solution, but, because the disodium salt prepared by the method disclosed in the prior art has strong hygroscopicity and poor stability, it is unfavorable for the preparation of freeze-dried powder preparation, seriously affecting formulation quality

Method used

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  • Disodium tedizolid phosphate and preparation method thereof
  • Disodium tedizolid phosphate and preparation method thereof
  • Disodium tedizolid phosphate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1 Preparation of tedizolid phosphate disodium salt according to the present invention

[0035] Material name

molecular weight

Feed amount (g)

moles

The molar ratio of

Tedizolid Phosphate

450

1

0.0022

1

Sodium triphenylmethyl Ph 3 CNa

266

1.55

0.0058

2.64

[0036] The preparation method comprises the steps of:

[0037] (1) Add 1g of tedizolid phosphate and 15ml of isopropanol to a 50ml single-necked bottle and stir at room temperature, add 15ml of 1.55g Ph 3 The diethyl ether solution of CNa was added dropwise in 40 minutes, and the reaction temperature was controlled at 40-45°C. During the reaction, the solution gradually changed from light red to white, monitored by TLC, and the reaction was stopped after 2 hours, and the resulting reaction solution was used for future use;

[0038] (2) The reaction solution obtained in step (1) was decolorized by adding 0.1 g of activated car...

Embodiment 2

[0041]Embodiment 2 Preparation of tedizolid phosphate disodium salt according to the present invention

[0042] Material name

molecular weight

Feed amount (g)

moles

The molar ratio of

Tedizolid Phosphate

450

2

0.0044

1

Sodium ethoxide EtONa

68

0.99

0.0146

3.32

[0043] The preparation method comprises the steps of:

[0044] (1) Add 2g of tedizolid phosphate and 20ml of ethanol to a 50ml single-mouth bottle and stir at room temperature, add 10ml of ethanol solution containing 0.99g of EtONa dropwise into a constant pressure dropping funnel, and finish adding dropwise in 30min, and control the reaction temperature at 40-45°C , during the reaction, the solution gradually changed from light yellow to white, monitored by TLC, and the reaction was stopped after 2 hours of raw material disappearance, and the resulting reaction solution was used for subsequent use;

[0045] (2) The reaction solution obtai...

Embodiment 3

[0047] Embodiment 3 Preparation of tedizolid phosphate disodium salt according to the present invention

[0048] Material name

molecular weight

Feed amount (g)

moles

The molar ratio of

Tedizolid Phosphate

450

2

0.0044

1

Sodium tert-butyl alkoxide t-BuONa

96

1.29

0.0134

3.04

[0049] The preparation method comprises the steps of:

[0050] (1) Add 2g of tedizolid phosphate and 25ml of tert-butanol to a 50ml single-mouth bottle and stir at room temperature, add 15ml of tert-butanol solution containing 1.29g t-BuONa dropwise through a constant pressure dropping funnel, dropwise for 40min, and the reaction temperature Control the temperature at 40-45°C. During the reaction, the solution gradually changes from light yellow to white, monitored by TLC, stop the reaction after 2 hours of raw materials disappear, and the obtained reaction solution is ready for use;

[0051] (2) Add 0.2 g of activated carbon...

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Abstract

The invention relates to disodium tedizolid phosphate and a preparation method thereof and belongs to the technical field of medicines. The X-ray powder diffraction pattern of disodium tedizolid phosphate shows that the characteristic absorption peaks appear when the reflection angles 2theta are 12.2+ / -0.2 degrees, 17.5+ / -0.2 degrees, 19.7+ / -0.2 degrees, 21.3+ / -0.2 degrees, 24.7+ / -0.2 degrees, 32.0+ / -0.2 degrees. The disodium tedizolid phosphate provided by the invention has excellent stability and purity and is very suitable for producing a freeze-dried powder injection as a raw material. In addition, the preparation method of disodium tedizolid phosphate is simple, is easy to operate, has the advantage of mild reaction condition, use of a small amount and a few kinds of organic solvents, is environment-friendly, is suitable for industrial production and is an environment-friendly preparation method.

Description

technical field [0001] The present invention relates to a medicine and a preparation method thereof, in particular to an oxazolidinone antibiotic tedizolid disodium phosphate, namely 3-[3-fluoro-4-[6-(2-methyl-2H- Disodium salt of tetrazol-5-yl)-3-pyridyl]phenyl]-5-(hydroxymethyl)-2-oxazolidinone phosphate and a preparation method thereof belong to the technical field of medicine. Background technique [0002] The widespread use of antibiotics has made the problem of bacterial resistance increasingly serious, and the research on new anti-drug-resistant bacteria has become the main direction of antibacterial drug research. Among them, linezolid, the first fully synthetic oxazolidinone antibacterial drug, has been successfully marketed and achieved good clinical results. [0003] [0004] Tedizolid Phosphate (Tedizolid Phosphate) is a second-generation oxazolidinone antibiotic developed by Dong-A Pharmaceutical, authorized to Cubist Pharmaceuticals and Bayer for commercial...

Claims

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Application Information

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IPC IPC(8): C07F9/6558
Inventor 张延峰马慧丽陈洁董朝蓬李永科薛子桥王博申洁
Owner 石药集团中诺药业(石家庄)有限公司
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