反应详情

温度

50 °C

To a solution of methyl 4-(1,1-dioxidotetrahydro-2H-1,2-thiazin-2-yl)-2,3-dihydro-1H-indole-6-carboxylate hydrochloride salt (D234) (350 mg, 1.0 mmol, 1 equiv) in AcOEt (5 ml) were added NEt3 (140 ml, 1.0 mmol, 1 equiv) and acetic anhydride (0.5 ml, 5.6 mmol, 5.6 equiv) and the resulting mixture was stirred at 50° C. for 30 min then cooled to room temperature and washed with a 2N aqueous HCl solution followed by a saturated aqueous NaHCO3 solution, then dried over MgSO4 and concentrated in vacuo to give methyl 1-acetyl-4-(1,1-dioxidotetrahydro-2H-1,2-thiazin-2-yl)-2,3-dihydro-1H-indole-6-carboxylate (D235) as a white solid which was used in the next step without further purification. [M+H]+=353.2, RT=2.24 min.

1. temperaturethen cooled to room temperature
2. washwashed with a 2N aqueous HCl solution
3. dry with materialdried over MgSO4
4. concentrationconcentrated in vacuo