反应详情

1-[3-({[tert-Butyl(dimethyl)silyl]oxy}methyl)-2-fluorophenyl]piperazine (140 mg) was mixed with DCE (4 ml), and ethanesulfonyl chloride (122 mg) and TEA (145 mg) were added thereto, followed by stirring at room temperature for 2 hours. CHCl3 and water were added to the reaction mixture, and the organic layer was dried over Na2SO4 and concentrated under reduced pressure. The obtained residue was mixed with THF (4 ml), and a 1M TBAF/THF solution (0.9 ml) was added thereto, followed by stirring at room temperature for 2 hours. EtOAc and water were added to the reaction mixture, and the organic layer was dried over Na2SO4 and concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (EtOAc/hexane) to obtain {3-[4-(ethylsulfonyl)piperazin-1-yl]-2-fluorophenyl}methanol (123.9 mg).

1. additionwere added
2. dry with materialthe organic layer was dried over Na2SO4
3. concentrationconcentrated under reduced pressure
4. additionThe obtained residue was mixed with THF (4 ml)
5. additiona 1M TBAF/THF solution (0.9 ml) was added
6. stirringby stirring at room temperature for 2 hours
7. additionEtOAc and water were added to the reaction mixture
8. dry with materialthe organic layer was dried over Na2SO4
9. concentrationconcentrated under reduced pressure
10. customThe obtained residue was purified by silica gel column chromatography (EtOAc/hexane)