(2S)-2-((Tetrahydro-2H-pyran-2-yl)oxy)propyl 4-methylbenzenesulfonate → (-)-4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-2-[1-(5-{[(2R)-2-hydroxypropyl]oxy}pyrimidin-2-yl)piperidin-4-yl]-7,7-dimethyl-5,6,7,8-tetrahydroquinolin-5-ol

Participants

Reaction Steps

Reactions similar to those of Example 37 were performed except for using (2R)-2-(tetrahydro-2H-pyran-2-yloxy)propyl 4-methylbenzenesulfonate, which was synthesized by the method described in B. A. Jones et al., Journal of Heterocyclic Chemistry, 1982, Vol. 19, pp. 551-556, instead of (2S)-2-(tetrahydro-2H-pyran-2-yloxy)propyl 4-methylbenzenesulfonate, and from 50 mg (77 μmol) of 4-(4,4-Difluorocyclohexyl)-3-{fluoro[4-(trifluoromethyl)phenyl]methyl}-2-[1-(5-hydroxy pyrimidin-2-yl)piperidin-4-yl]-7,7-dimethyl-5,6,7,8-tetrahydroquinolin-5-ol, which was prepared by a method similar to that of Example 4, 39 mg of the title compound was obtained as a white solid (yield: 71%).

Provenance & Evidence