反应详情

A suspension of tert-butyl (2-(4-((2S,4R)-1-acetyl-4-((5-cyanopyridin-2-yl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)benzamido)ethyl)carbamate (for a preparation see Intermediate 39)(65 mg, 0.114 mmol) in 1,4-dioxane (1 mL) at room temperature was treated with hydrogen chloride in 1,4-dioxane (4N, 2 mL, 8.00 mmol) and the resulting suspension was stirred at this temperature for 1 h then concentrated in vacuo. The precipitate formed was triturated with Et2O isolated by filtration and dried under vacuum to give 4-((2S,4R)-1-acetyl-4-((5-cyanopyridin-2-yl)amino)-2-methyl-1,2,3,4-tetrahydroquinolin-6-yl)-N-(2-aminoethyl)benzamide, hydrochloride (60 mg, 0.119 mmol, 104% yield) as a white solid. LCMS (HpH, 2 min), Rt=0.75 min, MH+=469.

1. customat room temperature
2. concentrationthen concentrated in vacuo
3. customThe precipitate formed
4. customwas triturated with Et2O
5. customisolated by filtration
6. customdried under vacuum