反应详情

温度

95 °C

To a solution of (S)-2-(7-bromo-2-chloro-5-methylbenzo[d]thiazol-6-yl)-2-tert-butoxyethyl pivalate (130 mg, 0.282 mmol) in dioxane, was added 3-benzyloxyphenylboronic acid pinacol ester (105 mg, 0.338 mmol), Pd(PPh3)4 (16 mg, 0.014 mmol), 2N K2CO3 (700 μL). The reaction mixture in sealed tube was heated at 95° C. for 1.5 hs. Then the reaction was cooled down. The reaction mixture was washed by sat. NaHCO3, and extracted by EtOAc. The organic phase was filtered, concentrated down, purified by silica gel column, eluting by 0-50% EtOAc in hexanes to give the product (100 mg, 58%). LCMS-ESI+: calc'd for C32H36BrNO4S: 610.2 (M+H+); Found: 610.2 (M+H+).

1. temperatureThen the reaction was cooled down
2. washThe reaction mixture was washed by sat. NaHCO3
3. extractionextracted by EtOAc
4. filtrationThe organic phase was filtered
5. concentrationconcentrated down
6. custompurified by silica gel column
7. washeluting by 0-50% EtOAc in hexanes