A simple and efficient strategy for direct regioselective esterification at O-2 of β-cyclodextrin was developed by using the combination of N, N'-carbonyldiimidazole and carbonate buffer in 1, 4-dioxane, which does not require large amounts of polar organic solvents such as DMF, toxic solvents such as CH3CN, or flammable bases such as NaH. Moreover, their hydrolyses by neighboring-group participation were observed. Mono-2-tosyl-β- ...