反应详情

温度

100 °C

To a solution of (S)-ethyl 2-tert-butoxy-2-(7-(4-chlorophenyl)-2-(2-chloropyridin-4-yl)-5-methylbenzo[d]thiazol-6-yl)acetate (32.0 mg, 0.061 mmol) and 7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one (20.0 mg, 0.073 mmol) in dioxane (0.5 mL) was added Pd(PPh3)4 (3.5 mg, 0.003 mmol) and 2N K2CO3 (127 μL, 0.255 mmol). The reaction was degassed for 5 minutes with N2 and then heated at 100° C. for 10 h. After cooling, the reaction mixture was diluted with EtOAc, extracted with H2O, brine, dried over Na2SO4, filtered and concentrated and purified by flash column chromatography (silica gel, 0 to 100% ethyl acetate/hexanes) to give the desired product. LCMS-ESI+ (m/z): [M+H]+ calcd for C34H32ClN4O5S: 643.2; found: 643.3.

1. customThe reaction was degassed for 5 minutes with N2
2. temperatureAfter cooling
3. additionthe reaction mixture was diluted with EtOAc
4. extractionextracted with H2O, brine
5. dry with materialdried over Na2SO4
6. filtrationfiltered
7. concentrationconcentrated
8. custompurified by flash column chromatography (silica gel, 0 to 100% ethyl acetate/hexanes)