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Pharmaceutical crystal of contezolid acefosamil as well as preparation method and application thereof

A technology of crystals and compounds, applied to the pharmaceutical crystals of contezolid and the fields of preparation and application thereof, can solve the problems of easy decomposition, poor stability and the like, and achieve the effect of improving stability

Active Publication Date: 2020-04-21
SHANGHAI MICURX LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, according to the preparation method of contezolid provided in this published text, whether it is traditional laboratory operation processing such as extraction, desolvation under reduced pressure, or HPLC purification and lyophilization of the obtained product, the X-ray powder diffraction analysis is between 0 and No diffraction peaks were shown between 40°2θ ( figure 1 ), are all amorphous powders, poor stability, easy to cause decomposition

Method used

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  • Pharmaceutical crystal of contezolid acefosamil as well as preparation method and application thereof
  • Pharmaceutical crystal of contezolid acefosamil as well as preparation method and application thereof
  • Pharmaceutical crystal of contezolid acefosamil as well as preparation method and application thereof

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preparation example Construction

[0062] Also disclosed herein are methods for preparing the above-mentioned crystals or crystal compounds. In some embodiments, the compound of formula I (crude product of contezolid amide ester of formula I) is dissolved in a mixed solution of organic solvent and water; inorganic salt is added, and then the product phase is separated), and part or all of the volatile Substance, adding organic solvent, crystallization to obtain crystals. The crude product of contezolid of formula I can be prepared by the method disclosed in CN105612166A.

[0063] The proportional volume ratio of the organic solvent and water is preferably 1:9 to 4:6.

[0064] In some embodiments, the organic solvent can be selected from acetonitrile, acetone, methanol, ethanol, propanol, isopropanol, butanol, ethyl acetate, isopropyl acetate, n-heptane, hexane, cyclohexane, petroleum At least one of ether, methyl ethyl ketone, and tetrahydrofuran.

[0065] In a more preferred embodiment, the organic solvent ...

Embodiment 1

[0086] synthetic route:

[0087]

[0088] Compound of Example 1: Under nitrogen protection, trimethyliodosilane (14.4g) was added dropwise to DCM (105mL) of Intermediate 1 (10.5g, prepared according to the method of CN105612166A Intermediate 2) at 0-10°C The solution was stirred at room temperature for 2 hours. The reaction solution was concentrated under reduced pressure, and the residue was rinsed with methyl tert-butyl ether (100 ml), filtered, and dried in vacuo. The resulting product was redissolved in DMSO / MeCN (10.5ml / 105ml), NaOAc (36.7g) and Ac 2 O (5.9 g), stirred for 1 hour. MTBE (700ml) was added, stirred, filtered, and dried in vacuo to obtain the crude compound of Example 1.

[0089] Example 1 Product Form 1: The crude product of Example 1 was stirred in 5% EtOH / DCM (1000ml), filtered, and the mother liquor was concentrated under reduced pressure. The residue was slurried with ethyl acetate:methyl tert-butyl ether (3:1, 300ml). Filter, wash (residue with ...

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Abstract

The invention provides a pharmaceutical crystal of contezolid acefosamil as well as a preparation method and application of the pharmaceutical crystal, particularly a crystal or crystal complex of a compound of formula I in which R is selected from hydrogen, sodium or a complex thereof in any proportion.

Description

technical field [0001] The invention provides a pharmaceutical crystal of contezolid acefosamil, a preparation method and application thereof. Background technique [0002] Oxazolidinone compounds are a new class of synthetic compounds with activity against various pathogenic microorganisms. The first drug of its kind, Linezolid, has been approved for the treatment of Gram-positive infections. Linezolid has good antibacterial activity, but as noted in the "Warnings" section of the prescribing instructions for linezolid, myelosuppression and amine oxidase inhibition are the main factors that limit the application of linezolid. Chinese patent publication CN105612166A discloses that contezolidinone is a new oxazolidinone compound with excellent safety characteristics and good antibacterial activity. [0003] In addition to the desired antimicrobial activity and safety, effective antimicrobials must possess solubility and stability suitable for practical applications. Chinese...

Claims

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Application Information

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IPC IPC(8): C07F9/6558A61K31/675A61P31/04
CPCC07F9/65583A61P31/04A61P31/00C07B2200/13C07F9/6558A61K31/675A61K31/664
Inventor 张学亮王星海刘进前M·F·高德福
Owner SHANGHAI MICURX LTD
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