反应详情

温度

120 °C

(R)-5-Bromo-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)nicotinamide (Stage 171.1, 50 mg, 0.108 mmol), 4-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile (32 mg, 0.130 mmol), PdCl2(dppf) (7.91 mg, 10.81 μmol) and K3PO4 (68.8 mg, 0.324 mmol) were added to a vial and flushed with argon. Dioxane (1 mL) was added and the mixture was stirred at 120° C. for 1.5 h. The solvent was evaporated off under reduced pressure and the crude product was purified by preparative SFC (Column 2-EP, from 17% to 22% in 6 min). The purified product was lyophilized in water/min. vol. MeCN to afford the title product as a slightly yellow powder. UPLC-MS (Condition 3), tR=1.09 min, m/z=503.1/505.2 [M+H]+.

1. customflushed with argon
2. additionDioxane (1 mL) was added
3. customThe solvent was evaporated off under reduced pressure
4. customthe crude product was purified by preparative SFC (Column 2-EP, from 17% to 22% in 6 min)