Novel voriconazole intermediate and synthesis of voriconazole

摘要

The present invention relates to a process for preparing a compound represented by the following general formula (1): (1) synthesizing a compound represented by the following general formula (3) by reacting a compound represented by the following general formula (4) 2) removing the thiol group and the chloro group which are substituents in the compound of Formula 3 to obtain racemate boricconazole of Formula 2; And 3) optically separating the racemic compound of formula (2) using an optically active acid. (In the above formulas, R is phenyl, pyridine, pyrimidine, thiazole, benzothiazole, benzoxazole, imidazole, 1-methylimidazole, C ₁ -C ₄ alkyl or substituents of these compounds, And is at least one selected from halo, nitro and methoxy.