反应详情

A mixture of 4-(6-Bromo-imidazo[1,2-a]pyrazin-8-ylamino)-benzoic acid (7) (0.16 mmol), benzotriazol-1-yloxy-tris(dimethylamino)-phosphonium hexafluorophosphate (0.16 mmol), and N′N-diisopropylethylamine (0.48 mmol) is stirred at room temperature for 20 min. under N2. Morpholine (0.48 mmol) is added and the mixture is stirred at room temperature for 16 hr. Water (10 mL) is added and the mixture extracted with ethyl acetate (2×70 mL). The extracts are subsequently washed with water (2×30 mL) and brine (1×30 mL), dried over sodium sulfate, and concentrated in vacuo. The residue is triturated with diethyl ether to give [4-(6-Bromo-imidazo[1,2-a]pyrazin-8-ylamino)-phenyl]-morpholin-4-yl-methanone (8) as a cream solid.

1. stirringthe mixture is stirred at room temperature for 16 hr
2. extractionthe mixture extracted with ethyl acetate (2×70 mL)
3. washThe extracts are subsequently washed with water (2×30 mL) and brine (1×30 mL)
4. dry with materialdried over sodium sulfate
5. concentrationconcentrated in vacuo
6. customThe residue is triturated with diethyl ether