Process for preparing voriconazole
US8263769B2 · kind B2 · utility
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7Claims
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Key dates
| Filing date | Aug 4, 2008 |
| Grant date | Sep 11, 2012 |
| Priority date | — |
| Expiry date | May 7, 2029 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.