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Pharmaceutical crystal of contezolid and its preparation method and application

A technology of crystals and compounds, which is applied in the pharmaceutical crystals of contezole carbamate and its preparation and application, can solve the problems of easy decomposition and poor stability, and achieve the effect of improving stability

Active Publication Date: 2022-06-07
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 and its preparation method and application
  • Pharmaceutical crystal of contezolid and its preparation method and application
  • Pharmaceutical crystal of contezolid and its preparation method and application

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[0062] Also disclosed herein are methods for preparing the above crystals or crystal compounds. In some embodiments, the compound of formula I (the crude product of contazolamide of formula I) is dissolved in a mixed solution of an organic solvent and water; an inorganic salt is added, and then the product phase is separated) to remove part or all of the volatility substance, add an organic solvent, and crystallize to obtain crystals. The crude product of contazolamide of formula I can be prepared by the method disclosed in CN105612166A.

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

[0064] In some embodiments, the organic solvent may 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 can be select...

Embodiment 1

[0086] synthetic route:

[0087]

[0088] Compound of Example 1: Trimethyliodosilane (14.4 g) was added dropwise to Intermediate 1 (10.5 g, prepared according to the method of CN105612166A Intermediate 2) in DCM (105 mL) at 0-10°C under nitrogen protection 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 were added 2 O (5.9 g), stirred for 1 hour. MTBE (700 ml) 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 (1000 ml), 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 (...

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Abstract

The invention provides drug crystals of contezolid and its preparation method and application. A crystal or crystal compound of a compound of formula I, wherein R is selected from hydrogen, sodium or a compound thereof in any ratio,

Description

technical field [0001] The invention provides a medicine crystal of contezolid acefosamil, a preparation method and application thereof. Background technique [0002] Oxazolidinones are a new class of synthetic compounds with activity against a variety of 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 myelosuppression and amine oxidase inhibition are the main factors limiting the use of linezolid, as noted in the Warnings section of the linezolid drug prescribing instructions. Chinese patent publication CN105612166A discloses that contazolamide is a new oxazolidinone compound with excellent safety characteristics and good antibacterial activity. [0003] In addition to the desired antibacterial activity and safety, an effective antibacterial drug must possess solubility and stability suitable for practical applications. Chinese Patent Publicat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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