反应详情

3-Benzyloxy-9-bromo-2-[5-(4-fluoro-benzyl)-thiazol-2-yl]-7-morpholin-4-yl-pyrido[1,2-a]pyrimidin-4-one (product of example 218, 110 mg, 0.18 mmol), 1-isopropyl-imidazolidin-2-one (30 mg, 0.22 mmol), Pd2(dba)3 (15 mg, 0.02 mmol), Xantphos (15 mg, 0.2 mmol), Cs2CO3 (58.5 mg, 0.18 mmol) were mixed in anhydrous dioxane (5 ml). The mixture was heated at 90° C. under the atmosphere of N2 for 4 h, after which water was added and then extracted with ethyl acetate. The extracts were combined, washed with brine, dried over sodium sulfate and evaporated under reduced pressure. The residue was purified by column chromatography to give the desired product (95 mg, yield 81%).

1. extractionextracted with ethyl acetate
2. washwashed with brine
3. dry with materialdried over sodium sulfate
4. customevaporated under reduced pressure
5. customThe residue was purified by column chromatography