反应详情

HCl (4M in 1,4-dioxane, 2 mL, 8 mmol) was added to a solution of 1-methylethyl((2S,4R)-1-acetyl-6-{1-[2-({[(1,1-dimethylethyl)oxy]carbonyl}amino)ethyl]-1H-1,2,3-triazol-4-yl}-2-methyl-1,2,3,4-tetrahydro-4-quinolinyl)carbamate (for a preparation, see intermediate 77) (108 mg, 0.22 mmol) in 1,4-dioxane (0.5 mL). The mixture was stirred at room temperature for 16 h. Et2O (5 mL) was added and the mixture stirred for 1 h. The solid formed was filtered off, washed with Et2O and dried under house vacuum to give 1-methylethyl {(2S,4R)-1-acetyl-6-[1-(2-aminoethyl)-1H-1,2,3-triazol-4-yl]-2-methyl-1,2,3,4-tetrahydro-4-quinolinyl}carbamate hydrochloride (75 mg, 0.172 mmol, 80%) as a colourless solid. LCMS (method G): Retention time 0.55 min, [M+H]+=401.1

1. customfor a preparation
2. stirringthe mixture stirred for 1 h
3. customThe solid formed
4. filtrationwas filtered off
5. washwashed with Et2O
6. customdried under house vacuum