反应详情

温度

90 °C

A suspension of 7-chloro-5-(methylthio)imidazo[1,2-c]pyrimidine hydrochloride (1.85 g, 7.83 mmol; Preparation H, Step A), 4-morpholinophenylboronic acid (1.78 g, 8.62 mmol) and potassium phosphate (3.33 g, 15.7 mmol) in isopropanol (25 mL) was purged with argon for 5 minutes, and then Pd2dba3 (0.717 g, 0.783 mmol) and XPHOS (1.49 g, 3.13 mmol) were added. The reaction was again purged for 5 minutes with argon before being sealed and heated to 90° C. for 18 hours. The reaction mixture was diluted with EtOAc (75 mL) and filtered. The filtrate was concentrated under reduced pressure, and the residue obtained was purified by silica gel column chromatography, eluting with 10-15-20% acetone in DCM to afford 4-(4-(5-(methylthio)imidazo[1,2-c]pyrimidin-7-yl)phenyl)morpholine (0.663 g, 25.9% yield) as a yellow solid. MS (apci) m/z=327.1 (M+H).

1. customwas purged with argon for 5 minutes
2. customThe reaction was again purged for 5 minutes with argon
3. custombefore being sealed
4. additionThe reaction mixture was diluted with EtOAc (75 mL)
5. filtrationfiltered
6. concentrationThe filtrate was concentrated under reduced pressure
7. customthe residue obtained
8. customwas purified by silica gel column chromatography
9. washeluting with 10-15-20% acetone in DCM