08-01-2015 дата публикации
Номер: US20150011757A1
Принадлежит:
Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. 4. The process according to claim 1 , wherein the cyclization reaction is performed in the presence of a catalyst claim 1 , preferably claim 1 , the catalyst is a Lewis acid or a mixture thereof.5. The process according to claim 4 , the catalyst is selected from lithium bromide claim 4 , magnesium bromide claim 4 , lithium chloride claim 4 , magnesium chloride claim 4 , magnesium iodide claim 4 , lithium iodide claim 4 , lithium chloride claim 4 , zinc chloride claim 4 , tetra-n-butylammonium bromide claim 4 , tetra-n-butylammonium chloride claim 4 , or any mixture thereof.6. The process according to claim 4 , the catalyst is selected from lithium bromide claim 4 , magnesium bromide claim 4 , magnesium iodide claim 4 , or any mixture thereof.7. The process according to claim 1 , wherein the cyclization reaction is performed in a solvent claim 1 , preferably claim 1 , the solvent is an aprotic solvent or a mixture thereof.8. The process according to claim 7 , the aprotic solvent includes but not limited to petroleum ether claim 7 , ethyl acetate claim 7 , isoamyl acetate claim 7 , butyl acetate claim 7 , toluene claim 7 , xylene claim 7 , chlorobenzene claim 7 , tetrahydrofuran claim 7 , dichloromethane claim 7 , N claim 7 ,N-dimethylformamide claim 7 , C-Calkanes claim 7 , acetone claim 7 , 1 claim 7 ,4-dioxane claim 7 , acetonitrile claim 7 , or any mixture thereof.9. The process according to claim 1 , wherein the temperature of the cyclization reaction is in the range of 60° C.-150° C.10. The process according to claim 9 , wherein the temperature of ...
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