反应详情

4-(4-(5-(1H-Pyrazol-4-yl)imidazo[1,2-c]pyrimidin-7-yl)phenyl)morpholine (0.0300 g, 0.0866 mmol) and 3-cyclopentylaerylonitrile (Table 1, compound g; 0.0175 g, 0.144 mmol) were suspended in DMF (3 mL) and 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine (0.0324 mL, 0.217 mmol) added in one portion. The reaction mixture was stirred at ambient temperature over the weekend. The reaction mixture was partitioned between saturated aqueous 1 N NaOH and EtOAc. The solids were isolated by filtration. The organics were washed with brine, dried over MgSO4 and concentrated under reduced pressure to afford the crude material, which was purified by flash column chromatography (eluant: 0.5-3% (9:1, MeOH:NH4OH)/DCM) to provide 3-cyclopentyl-3-(4-(7-(4-morpholinophenyl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)propanenitrile (0.0190 g, 0.04064 mmol, 46.9% yield). MS (apci) m/z=468.2 (M+H).

1. customThe reaction mixture was partitioned between saturated aqueous 1 N NaOH and EtOAc
2. customThe solids were isolated by filtration
3. washThe organics were washed with brine
4. dry with materialdried over MgSO4
5. concentrationconcentrated under reduced pressure
6. customto afford the crude material, which
7. customwas purified by flash column chromatography (eluant: 0.5-3% (9:1, MeOH:NH4OH)/DCM)