反应详情

温度

110 °C

6-(2-Chloro-4-isopropoxy-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylbenzo[d]oxazole (1 equiv), 4-amino-3-methoxy-N-methylbenzamide (1.2 equiv), palladium acetate (0.1 equiv), 2,2′-bis(diphenylphosphino)-1,1′-binaphthalene (0.2 equiv), cesium carbonate (5 equiv), and 1,4-dioxane (0.14 M) were combined and allowed to stir at 110° C. for 4 h and then cool to ambient temperature overnight. The reaction mixture was diluted with ethyl acetate and filtered through a pre-wetted (with ethyl acetate) bed of Celite. The filtrate was concentrated to an oil under reduced pressure that was purified by silica gel chromatography (0-70% ethyl acetate with 10% methanol/hexane) to afford the title compound (82% yield). MS (ESI) m/z 617.5 [M+1]+.

1. temperaturecool to ambient temperature overnight
2. filtrationfiltered through a pre-wetted (with ethyl acetate) bed of Celite
3. concentrationThe filtrate was concentrated to an oil under reduced pressure that
4. customwas purified by silica gel chromatography (0-70% ethyl acetate with 10% methanol/hexane)