反应详情

温度

60 °C

To a mixture of 6-amino-adamantane-1,3-diol hydrochloride (258 mg, J. Med. Chem. 50, 2007, 149), N-Boc-cycloleucinal (250 mg) and acetic acid (0.67 ml) in MeOH (5.0 ml), sodium triacetoxyborohydride was added at room temperature. The mixture was stirred at 60° C. for 30 min. The mixture was basified with saturated NaHCO3 solution. The mixture was extracted with AcOEt, washed with brine, dried over MgSO4 and evaporated. The residue was purified with silica gel chromatography (CH2Cl2:MeOH:NH4OH=from 100:0:0 to 90:9:1) to obtain the title compound (250 mg, 56%) as a white amorphous.

1. additionwas added at room temperature
2. extractionThe mixture was extracted with AcOEt
3. washwashed with brine
4. dry with materialdried over MgSO4
5. customevaporated
6. customThe residue was purified with silica gel chromatography (CH2Cl2:MeOH:NH4OH=from 100:0:0 to 90:9:1)