反应详情

A solution of 1-methylethyl((2S,4R)-1-acetyl-6-{1-[3-({[(1,1-dimethylethyl)oxy]carbonyl}amino)propyl]-1H-1,2,3-triazol-4-yl}-2-methyl-1,2,3,4-tetrahydro-4-quinolinyl)carbamate (for a preparation, see Intermediate 73) (543 mg, 1.055 mmol) in 1,4-dioxane (1 mL) was treated with HCl (4N in 1,4-dioxane, 4.00 mL, 16 mmol) and the resulting mixture was stirred for 2 h at room temperature then concentrated in vacuo. The residue was co-evaporated twice with toluene then triturated with Et2O and filtered off to give 1-methylethyl {(2S,4R)-1-acetyl-6-[1-(3-aminopropyl)-1H-1,2,3-triazol-4-yl]-2-methyl-1,2,3,4-tetrahydro-4-quinolinyl}carbamate hydrochloride (370 mg, 0.771 mmol, 73% yield) as a brown solid.

1. concentrationthen concentrated in vacuo
2. customthen triturated with Et2O
3. filtrationfiltered off