Preparation of optically active 5-hydroxy-3-ketoalkanoic acid ester derivatives used as intermediates for drugs, especially tipranavir, by optical resolution of racemate by preparative high performance liquid chromatography

摘要

Preparation of optically active 5-hydroxy-3-ketoalkanoic acid ester derivatives (I) comprises subjecting the corresponding racemic mixture of compounds (II) to preparative high performance liquid chromatography (HPLC) on a chiral carrier. Preparation of optically active 5-hydroxy-3-ketoalkanoic ester derivatives of formula (I) comprises subjecting the corresponding racemic mixture of compounds of formula (II) to preparative HPLC on a chiral carrier. R1, R2 = H or 1-8C alkyl, 3-8C cycloalkyl, 6-10C aryl or (6-10C) aryl-(1-8C) alkyl (all optionally substituted by 1-3 OH, halo, 1-4C alkoxy or CF3), and R3 = 1-8C alkyl, 1-4C haloalkyl, (6-10C) aryl-(1-8C) alkyl or trihydrocarbylsilyl. provided that R1 and R2 are different.