反应详情

The title compound was prepared from 3-[6′-methyl-4′-(4-trifluoromethyl-phenyl)-[2,2′]bipyridinyl-6-yl]-benzenesulfonyl chloride (example 1.2) (0.465 g, 0.951 mmol) by treatment with commercially available 4-aminotetrahydropyran [CAS-no. 38041-19-9] (0.192 g, 1.9 mmol) in THF (5 ml) at 23° C. for 16 h. Diluted with EtOAc, washed with 5% citric acid, sat. NaHCO3-sol. and brine, dried organic layer over Na2SO4. Removal of the solvent in vacuum left a crude product, which was purified by silica gel column chromatography with EtOAc followed by trituration with diethyl ether/heptane to give the title compound (0.460 g, 87%) as an off-white solid. MS (ISP) 554.2 [(M+H)+]; mp 163° C. (dec.).

1. washwashed with 5% citric acid, sat. NaHCO3-sol
2. customRemoval of the solvent in vacuum
3. waitleft a crude product, which
4. customwas purified by silica gel column chromatography with EtOAc