反应详情

The product of step A (60 mg, 0.16 mmol), sodium azide (13 mg, 0.2 mmol), trimethyl orthoformate (0.3 mL, 2.7 mmol), and acetic acid (0.15 mL, 2.6 mmol) were heated at 80° C. for 6 hours. The solution was cooled and diluted with water. The solution was neutralized with NaHCO3 and extracted with DCM. The organic layers were dried (Na2SO4), filtered, and concentrated. The residue was purified via reverse-phase HPLC (C18: gradient 10-100 water/acetonitrile 0.1% formic acid) which yielded the title compound. MS (ESI) m/z 420 [M+H]+. GPR119 Human EC50: 0.07 nM

1. temperatureThe solution was cooled
2. extractionextracted with DCM
3. dry with materialThe organic layers were dried (Na2SO4)
4. filtrationfiltered
5. concentrationconcentrated
6. customThe residue was purified via reverse-phase HPLC (C18: gradient 10-100 water/acetonitrile 0.1% formic acid) which