Process for preparing voriconazole
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United States of America Patent
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Sep 11, 2012
Grant Date -
Jul 29, 2010
app pub date -
Aug 4, 2008
filing date -
Aug 6, 2007
priority date (Note) -
Expired
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Abstract
Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid.
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