反应详情

6-Bromoquinazolin-4(3H)-one Compound 178-A (1.0 g), 2-bromoethanol (1.1 g), and potassium carbonate (610 mg) were heated in DMA (10 mL) at 80° C. for 16 h. Reaction was extracted with water and dichloromethane (3 times), combined organic layers washed with brine, over sodium sulphate and concentrated. Residue was triturated with acetonitrile to yield 6-bromo-3-(2-hydroxyethyl)quinazolin-4(3H)-one Compound 178-B (810 mg) as a white solid. MS m/z (ESI)=268.9 (base peak, 79Br−M+H+); 270.9 (81Br−M+H+); 290.9 (79Br−M+Na+); 292.9 (81Br−M+Na+).

1. customReaction
2. extractionwas extracted with water and dichloromethane (3 times)
3. washwashed with brine, over sodium sulphate
4. concentrationconcentrated
5. customResidue was triturated with acetonitrile