PROCESSES FOR THE PREPARATION OF LINEZOLID INTERMEDIATE

摘要

The present invention provides improved methods of converting R-N-(4-morpholiyl- 3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl azide (III) to the intermediate S-N-(4- morpholinyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl amine (II) that involve the production of fewer by-products than previous methods. The amine (II) may then be converted into linezolid (I) of high chemical purity with respect to the inactive R- enantiomer and bis-linezolid (IV), and is in high yield, without the need for tedious, complicated purification steps, such as chromatography.