Evaporation crystallization process for linezolid with crystal form I

A technology of linezolid and evaporation crystallization, which is applied in the field of compound synthesis technology, can solve problems such as difficulty in realizing industrial production, low yield, and difficult solvent recovery, and achieve low solvent usage, high yield, and fast evaporation speed Effect
CN102070548AActive Publication Date: 2011-05-25ZHEJIANG LEPU PHARMA CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG LEPU PHARMA CO LTD
Publication Date
2011-05-25

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Abstract

The invention discloses an evaporation crystallization process for linezolid with crystal form I. The method comprises the steps of: dissolving 1 weight part of linezolid in 3 to 5 weight parts of alcohol solvents, evaporating 60 to 70 weight percent of alcohol solvents at the temperature of between 70 and 100 DEG C, inducing crystal nuclei of the linezolid with crystal form I in a boiling state,reducing the temperature by 10 to 20 DEG C, adding the evaporated alcohol solvents again, precipitating crystals, filtering, washing a filter cake by using n-heptane, and performing vacuum-drying at the temperature of between 40 and 50 DEG C and under the pressure of -0.08 to -0.09 MPa to obtain the linezolid with crystal form I. In the evaporation process, the using amount of the solvents is small, the evaporation speed is high, evaporated liquor does not contain crystals, and the evaporated liquor can be directly recycled; and the linezolid is not decomposed and deteriorated, yield is high and the quality is good.
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Description

technical field

[0001] The present invention relates to a compound synthesis process, in particular to an evaporation crystallization process of crystal form I linezolid. Background technique

[0002] Linezolid, chemical name: [(S)-N-[[3-(3-fluoro-4morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methylacetamide], It is an antibacterial drug used for skin infections caused by various bacteria. Molecular formula is C 16 h 20 FN 3 o 4 , has the following structure (1):

[0003]

[0004] (1)

[0005] U.S. Patent No.5688792, European Patent No.717738, Israeli Patent No.110802, Canadian Patent No.2168560, International Patent WO95 / 07171 and Chinese Patents CN 101128442, CN101220001, CN101774978, document J. Med. Chem. 39(3) 673-679, 1996; Tetrahedron Lett., 40(26)4855,1999; Chinese Journal of Pharmaceutical Industry, 2010(41) 1, 61-62, disclosed linezolid and its preparation method.

[0006] Linezolid has multiple crystal forms, and it is generally believed that there are thre...

Claims

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