反应详情

4.2 g (7.61 mmol) of diethyl 2-(4-tert-butoxycarbonylaminobutyl)-2-[1-(toluene-4-sulfonyl)-1H-imidazol-4-yl]malonate were dissolved in 190 ml of methanol and stirred with 4.66 g (30.45 mmol) of 1-hydroxybenzotriazole hydrate at RT for 1 h. The reaction mixture was concentrated under reduced pressure, and the residue was chromatographed on silica gel (CH2Cl2:MeOH 9:1). The product-containing fractions were concentrated and the oil obtained was dissolved in ethyl acetate and washed with saturated NaHCO3 solution. The organic phase was dried over Na2SO4, filtered and concentrated. This gave 2.14 g (71%) of the title compound.

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. customthe residue was chromatographed on silica gel (CH2Cl2:MeOH 9:1)
3. concentrationThe product-containing fractions were concentrated
4. customthe oil obtained
5. washwashed with saturated NaHCO3 solution
6. dry with materialThe organic phase was dried over Na2SO4
7. filtrationfiltered
8. concentrationconcentrated