反应详情

A solution of 1-methylethyl {(2S,4R)-1-acetyl-6-[4-({[2-({[(1,1-dimethylethyl)oxy]carbonyl}amino)ethyl]amino}carbonyl)phenyl]-2-methyl-1,2,3,4-tetrahydro-4-quinolinyl}carbamate (for a preparation see Intermediate 37)(90 mg, 0.163 mmol) in dioxane (2 ml) was treated with hydrogen chloride in 1,4-dioxane (4N, 2 mL, 8.00 mmol) and the resulting mixture stirred at room temperature for 5 h, then concentrated in vacuo. The resulting residue was triturated with Et2O and isolated by filtration to give isopropyl ((2S,4R)-1-acetyl-6-(4-((2-aminoethyl)carbamoyl)phenyl)-2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)carbamate hydrochloride (68 mg, 0.139 mmol, 85% yield) as a pale yellow solid. LCMS (HpH, 2 min), Rt=0.78 min.

1. concentrationconcentrated in vacuo
2. customThe resulting residue was triturated with Et2O
3. customisolated by filtration