反应详情

温度

85 °C

Methyl (S)-1-((S)-2-(7-bromo-1H-naphtho[1,2-d]imidazol-2-yl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-ylcarbamate (482 mg, 1.02 mmol) and (1R,3S,4S)-tert-butyl 3-(7-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4,5-dihydro-1H-naphtho[1,2-d]imidazol-2-yl)-2-azabicyclo[2.2.1]heptane-2-carboxylate (552 mg, 1.12 mmol) were combined in DME (12 mL). Pd(PPh3)4 (118 mg, 0.102 mmol) and K2CO3 (2M H2O, 1.68 mL, 3.36 mmol) were added, and the solution was degassed with N2 for 10 min. The solution was heated to 85° C. and stirred o/n. The following morning, the solution was cooled to rt. The solution was diluted with EtOAc, washed with sat. NaHCO3, brine, dried with MgSO4, and concentrated. The residue was purified by silica gel chromatography to yield product (307 mg).

1. customthe solution was degassed with N2 for 10 min
2. temperatureThe following morning, the solution was cooled to rt
3. additionThe solution was diluted with EtOAc
4. washwashed with sat. NaHCO3, brine
5. dry with materialdried with MgSO4
6. concentrationconcentrated
7. customThe residue was purified by silica gel chromatography