反应详情

温度

95 °C

The reaction mixture of (S)-methyl 2-(2-bromo-7-(4-chlorophenyl)-5-methylbenzo[d]thiazol-6-yl)-2-tert-butoxyacetate (370 mg, 0.769 mol), 2-chloropyridine-4-boronic acid (157 mg, 0.99 mmol), 2N K2CO3 (1.9 mL), Pd(PPh3)4 (80 mg, 0.077 mmol) in dioxane (10 mL) was heated at 95° C. for 2 hrs. The reaction mixture was diluted by EtOAc, washed by sat. NaHCO3, extracted by EtOAc, the organic phase was dried over MgSO4, filtered, concentrated down and purified by silica gel column, eluting by 0-100% EtOAc in hexanes to give the product. LCMS-ESI+: calc'd for C26H24Cl2N2O3S: 515.1 (M+H+); Found: 515.1 (M+H+).

1. washwashed by sat. NaHCO3
2. extractionextracted by EtOAc
3. dry with materialthe organic phase was dried over MgSO4
4. filtrationfiltered
5. concentrationconcentrated down
6. custompurified by silica gel column
7. washeluting by 0-100% EtOAc in hexanes
8. customto give the product