Process for making linezolid

A technology of linezolid and oxazolidine, which is applied in the field of preparing compound linezolid, and can solve the problems of low yield, explosion hazard, harsh reaction conditions, etc.
CN103140487AInactive Publication Date: 2013-06-05SYNTHON BV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SYNTHON BV
Publication Date
2013-06-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention relates to a process for making the compound 3-(3-fluoro-4-(morpholin-4-yl)phenyl)-2-oxooxazolidin-5(S)-ylmethyl)amine of formula (II) and / or an acid addition salt thereof comprising: a) reacting the compound of formula (VII) wherein L is a leaving group, with a metal salt of diformylamide of formula (VIII) wherein Me+ is a sodium or potassium cation; and b) subjecting the reaction product of the step (a) comprising, alone or in admixture, compounds of formula (IXa) and / or (IXb), to a reaction with an acid. The invention further relates to a method for preparing linezolid by acetylation of the compound of formula (II).
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Description

Background of the invention

[0001] The present invention relates to an improved process for the preparation of the compound linezolid.

[0002] Linezolid is a pharmaceutically active compound that can be used as an antibacterial agent, for example, in the treatment of diabetic food infections caused by Gram-positive bacteria. Linezolid is represented by the following formula (I).

[0003]

[0004] Commercially available pharmaceutical compositions are sterile isotonic solutions for intravenous infusion, tablets for oral administration and aqueous suspensions for oral administration. They are marketed under the trade name ZYVOX by the company Pfizer.

[0005] The molecule of linezolid has an asymmetric carbon in the molecule, allowing the formation of two enantiomers; the commercially available compound is the (S)-enantiomer. In the above-mentioned commercially available compositions, linezolid exists in the form of free base.

[0006] Hereinafter, the name Linezolid wil...

Claims

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