反应详情

A solution of 1,1-dimethylethyl (1-{[(1R)-4,9-dioxo-1,2-dihydro-4H,9H-imidazo[1,2,3-ij]-1,8-naphthyridin-1-yl]methyl}-4-piperidinyl)carbamate (see Example 1 (i) above) (4.282 g, 10.69 mmol) in CHCl3 (20 ml) under Ar at room temperature was treated with HCl (4M solution in 1,4-dioxane, 20 ml, 80 mmol) and stirred at rt for 15 min, MeOH (20 ml) was then added. After stirred for 15 min, the reaction was evaporated and triturated with Et2O (20 ml). The obtained solid was dried in vacuo to give (1R)-1-[(4-amino-1-piperidinyl)methyl]-1,2-dihydro-4H,9H-imidazo[1,2,3-ij]-1,8-naphthyridine-4,9-dione dihydrochloride (4.55 g, 12.21 mmol, 100%) as a yellow powder.

1. customat room temperature
2. stirringAfter stirred for 15 min
3. customthe reaction was evaporated
4. customtriturated with Et2O (20 ml)
5. customThe obtained solid was dried in vacuo