反应详情

温度

90 °C

To a solution of (S)-ethyl 2-(2-bromo-7-(4-chlorophenyl)-5-methylbenzo[d]thiazol-6-yl)-2-tert-butoxyacetate (858 mg, 1.73 mmol) and 2-chloropyridine-4-boronic acid (327 mg, 2.08 mmol) in dioxane (14.6 mL) was added Pd(PPh3)4 (160 mg, 0.139 mmol) and 2N K2CO3 (3.6 mL, 7.28 mmol). The reaction was degassed for 5 minutes with N2 and then heated at 90° C. for 6 h. After cooling, the reaction mixture was diluted with EtOAc, extracted with H2O, brine, dried over Na2SO4, filtered, 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 C27H27Cl2N2O3S: 529.1; found: 529.2.

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)