反应详情

A mixture of 4-chloro-6-[2-(4-methyl-5-phenyl-1H-imidazol-2-yl)-4-morpholinyl]-2-pyrimidinamine (1.2 g, 3.24 mmol), 2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile (1.199 g, 4.85 mmol), Na2CO3 (0.857 g, 8.09 mmol) and Pd(PPh3)4 (0.374 g, 0.324 mmol) was placed into a microwave vial and heated in Biotage Initiator using initial 150 W to 140° C. for 1 hour. After cooling the reaction, the solvent was removed under reduced pressure, and the crude product was added to a silica gel column and eluted with Hex/EtOAc (1:3) to afford the title compound (1.2 g) as a yellow solid. LC-MS (ES) m/z=456 [M+H]+.

1. temperatureheated in Biotage Initiator
2. customfor 1 hour
3. temperatureAfter cooling
4. customthe reaction
5. customthe solvent was removed under reduced pressure
6. additionthe crude product was added to a silica gel column
7. washeluted with Hex/EtOAc (1:3)