反应详情

To a mixture of 6-[(1-amino-cyclopentylmethyl)-amino]-adamantane-1,3-diol (250 mg, obtained in examples 122, step B) and N,N-diisopropylethylamine (0.62 ml) in CH2Cl2 (3.0 ml), a solution of triphosgene (90 mg) in THF (1 ml) was added dropwise at room temperature. The mixture was stirred at room temperature for 2 hr. The mixture was poured into saturated NaHCO3 solution, and extracted with AcOEt. The organic layer was washed with brine, dried over MgSO4 and evaporated. The residue was triturated with CH2Cl2 to obtain the title compound (100 mg, 37%) as a white solid. MS (ESI): 307.1 (MH+).

1. extractionextracted with AcOEt
2. washThe organic layer was washed with brine
3. dry with materialdried over MgSO4
4. customevaporated
5. customThe residue was triturated with CH2Cl2