METHOD OF PRODUCING VORICONAZOLE Russian patent published in 2011 - IPC C07D403/06 C07D403/14 C07D239/30 C07D239/38 

Abstract RU 2434009 C1

FIELD: chemistry.

SUBSTANCE: described is a method of producing optically pure voriconazole via: a) coupling reaction of 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone with 4-(1-bromoethyl)-6-(4-chlorophenylsulphanyl)-5-fluoropyrimidine in Reformatsky reaction conditions to obtain the desired (2R,3S)/(2S,3R) enantiomeric pair, b) splitting the thiol fragment from the enantiomer to obtain racemic voriconazole; and c) extracting the desired optically pure voriconazole via optical separation of the enantiomer using an optically active acid.

EFFECT: improved method.

4 cl, 7 ex, 1 tbl

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RU 2 434 009 C1

Authors

Moon Joung-Kho

Li Moon Sub

Joo Dzae Kho

Kim Dzi Sook

Kim Khan Kiong

Choi Chang Dzu

Chang Joung Kil

Li Gvan Sun

Dates

2011-11-20Published

2008-08-04Filed