反应详情

温度

80 °C

To a solution of ((4-(tert-butylcarbamoyl)piperidin-1-yl)methyl)trifluoroborate (45 mg, 0.169 mmol) in THF/water 4:1 (3 mL) are added 6-trifluoromethyl-pyridine-2-carboxylic acid (6-chloro-pyrimidin-4-yl)-amide (51.2 mg, 0.169 mmol), palladium (II) acetate, (0.949 mg, 0.00423 mmol,), X-Phos, (2-dicyclohexylphosphino-2′,4′,6′-triisopropylbiphenyl) (4.84 mg, 0.0101 mmol) and Cs2CO3, (165 mg, 0.507 mmol). The mixture is purged with argon and is stirred overnight in a sealed tube at 80° C. The mixture is let to cool down. Water (3 mL) and AcOEt (5 mL) are added and the aqueous phase is extracted with AcOEt (10 mL). The organic phase is dried over MgSO4, filtered and evaporated. The residue is purified by prep HPLC E delivering the title compound (27 mg, 30%) as a white powder, LC-MS A: tR=0.74 min; [M+H]+=465.4.

1. customThe mixture is purged with argon
2. temperatureto cool down
3. additionWater (3 mL) and AcOEt (5 mL) are added
4. extractionthe aqueous phase is extracted with AcOEt (10 mL)
5. dry with materialThe organic phase is dried over MgSO4
6. filtrationfiltered
7. customevaporated
8. customThe residue is purified by prep HPLC E