反应详情

温度

140 °C

DIPEA (3.67 mL, 21.0 mmol) was added to (R)-5-Bromo-6-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 6.2, 2.77 g, 7.0 mmol) and 3-hydroxyazetidine HCl (0.920 g, 8.40 mmol) in iPrOH (7.0 mL) in a vial which was sealed and the RM mixture was stirred at 140° C. for 1.5 h. After cooling to RT, the RM was dissolved in EtOAc, washed with brine, dried over Na2SO4 and the solvent was evaporated off under reduced pressure to give the title product as a yellow foam. HPLC (Condition 4) tR=5.37 min, UPLC-MS (Condition 3) tR=1.09 min, m/z=432/434 [M+H]+.

1. customwas sealed
2. temperatureAfter cooling to RT
3. washwashed with brine
4. dry with materialdried over Na2SO4
5. customthe solvent was evaporated off under reduced pressure