- A PROCESS FOR MAKING VORICONAZOLE
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The present invention relates to a process of making a pair of trans-diastereomers of a compound of formula (I) comprising the step of reacting the compound of formula (VI) with an acid or a carboxylate salt thereof of formula (X) wherein M is hydrogen or an equivalent of a metal cation, in the presence of a metal salt in a solvent, and to the use of the compound (X) in making voriconazole.
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Page/Page column 13
(2011/10/05)
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- Structure and amide-amide tautomerism of 4-hydroxypyrimidines. Determination of the tautomeric composition by 13C NMR spectroscopy
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4-Hydroxypyrimidine and 5-fluoro-, 2-alkylthio-, and 2-amino-4-hydroxypyrimidines exist in solution as tautomeric mixtures of two oxo forms with conjugated and isolated double bonds in the heteroring, which can be regarded as cyclic amides. According to the 13C NMR data, the tautomer with isolated double bonds has a zwitterionic structure. Its fraction depends on the proton-donor power and dielectric constant of the solvent and the nature of the substituent in position 2. The tautomeric compositions were calculated on the basis of the intensity ratio of signals from the carbonyl carbon atoms, which turned out to be most sensitive to the tautomer structure. 2-Amino and 2-alkylthio groups were found to reduce the rate of exchange between the tautomeric forms.
- Kheifets,Kol'tsov,Khachaturov,Gindin
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p. 1373 - 1387
(2007/10/03)
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