反应详情

To a suspension of 3-chloro-4-(3,3,3-trifluoro-2-hydroxy-1-methyl-2-quinolin-3-yl-propyl)-phenol (Example 179, 55 mg) and cesium carbonate (52 mg) in N,N-dimethylacetamide (1 ml) was added benzenesulfonyl chloride (25 mg). After being stirred at room temperature for 2 days, more benzenesulfonyl chloride (14 mg) was added and the mixture was stirred at room temperature for 2 h. Water was added and the mixture was extracted with EtOAc. The organic phase was washed with brine and with water and dried (MgSO4). The product was purified by chromatography (SiO2, cyclohexane=>cyclohexane/EtOAc 1:1) to give the title compound (29 mg) as an off-white solid. MS (m/e)=522.2 [M+H+].

1. stirringthe mixture was stirred at room temperature for 2 h
2. extractionthe mixture was extracted with EtOAc
3. washThe organic phase was washed with brine and with water
4. dry with materialdried (MgSO4)
5. customThe product was purified by chromatography (SiO2, cyclohexane=>cyclohexane/EtOAc 1:1)