反应详情

温度

50 °C

To 1-(2-diethylaminoethyl)-3-hydroxy-3-(2-chlorophenyl)-4-bromo-6-iodooxindole (25.0 mg, 4.64×10−5 mol), 3-(2-oxo-1-imidazolidinyl)-1-propyne (8.6 mg, 1.5 eq.), Pd(PPh3)2Cl2 (4.88 mg, 15 mol %) and CuI (1.32 mg, 15 mol %) under a nitrogen atmosphere was added anhydrous Et3N (0.5 mL), anhydrous toluene (0.5 mL) and anhydrous THF (0.5 mL). The resulting yellow mixture was heated to 50° C. (bath temperature) and stirred at that temperature for 1 hour 20 minutes. The solvent was then removed in vacuo to give a yellow solid. Purification was carried out by column chromatography (silica gel, 6% MeOH in CHCl3) to yield the title compound (23.9 mg, 92%) as a light brown solid.

1. customThe solvent was then removed in vacuo
2. customto give a yellow solid
3. customPurification