反应详情

The product of example 54 (step A) (100 mg, 0.232 mmol), CuI (44 mg, 0.232 mmol), triazole (48 mg, 0.697 mmol), NaOtBu (67 mg, 0.697 mmol) and N,N′-dimethylethylene diamine (61 mg, 0.697 mmol) in NMP (1 mL) was heated at 130° C. for 15 h. The reaction was cooled to room temperature, diluted with EtOAc and washed with H2O (×3). The organic layer was dried over anhydrous MgSO4, filtered, and concentrated under vacuum to leave a residue which was purified by silica gel column chromatography (elution with 2:1 hexane:ethyl acetate) to yield the title compound. MS (ESI) m/z 419 [M+H]+. GPR119 Human EC50: 0.3 nM

1. washwashed with H2O (×3)
2. dry with materialThe organic layer was dried over anhydrous MgSO4
3. filtrationfiltered
4. concentrationconcentrated under vacuum
5. customto leave a residue which
6. customwas purified by silica gel column chromatography (elution with 2:1 hexane:ethyl acetate)