Preparation method of bacterial protein synthesis inhibitor linezolid crystal form III

Abstract

The invention discloses a preparation method of a bacterial protein synthesis inhibitor linezolid crystal form III. The bacterial protein synthesis inhibitor linezolid crystal form III is prepared byutilizing bacterial protein synthesis inhibitor linezolid. The preparation method has the advantages of concise preparation process, easiness in raw material obtaining, simple synthesis condition, economical property, environment friendliness, high product yield and high product purity; the industrialization is favorably realized, and the production cost is reduced; the preparation method of the bacterial protein synthesis inhibitor linezolid crystal form III is suitable for mass production; the sought novel preparation method of the bacterium protein synthesis inhibitor is quite meaningful for an economic technology of the linezolid. The bacterial protein synthesis inhibitor linezolid crystal form III prepared by the preparation method disclosed by the invention has the advantages of highoptical purity, can be used for treating methicillin-resistant staphylococcal infection and has important significance for studying the curative effects of solid drugs; the bioavailability of the bacterial protein synthesis inhibitor linezolid crystal form III can be improved, and the use of the bacterial protein synthesis inhibitor linezolid crystal form III in drug processing and drug combination is facilitated..

Description

Technical field [0001] The invention belongs to the field of pharmaceutical chemical synthesis, and in particular relates to a preparation method of linezolid crystal form III, a bacterial protein synthesis inhibitor. Background technique [0002] Linezolid is a bacterial protein synthesis inhibitor, which has good antibacterial effect on methicillin-sensitive or resistant Staphylococcus, vancomycin-sensitive or resistant Enterococcus, penicillin-sensitive or resistant Streptococcus pneumoniae, and has good antibacterial effect on anaerobic bacteria. With antibacterial activity. Unlike other drugs, linezolid does not affect peptidyl transferase activity. The site and mode of action of linezolid are unique, so in positive bacteria with intrinsic or acquired resistance characteristics, it is not easy to cross-resistance with other antibacterial drugs that inhibit protein synthesis, and it is not easy to induce bacterial resistance in vitro generation. The structural formula...

AI Technical Summary

Problems solved by technology

[0006] The preparation method of linezolid crystal form III reported in the literature and patents often uses high boiling point reagent toluene as a solvent. Since toluene is a second-class solvent, there is a certain risk in using toluene as a solvent for the preparation of crystal forms in pharmaceutical development.

In addition, ethyl acetate is also used as a crystallization solvent in the prior art, but the reaction process is complicated when using this solvent to prepare crystal form III, and it needs to have strict requirements on reaction conditions such as temperature, which is difficult for industrial application. It is necessary to develop a new Method for bacterial protein synthesis inhibitor linezolid crystal form III