反应详情

(g) 2-(4-(1-(4-Fluorophenyl)-1H-indazol-5-yl)tetrahydro-2H-pyran-4-yl)-2-methylpropanoic acid (50 mg, 0.13 mmol) was dissolved in 5 mL DCM, 32 uL pyridine, and treated with 27 uL cyanuric fluoride. After 1 h, the reaction was extracted from NaHCO3 with EtOAc×3. The combined organic layers were dried over MgSO4, filtered, concentrated and taken up in 2 mL NMP and treated with triethylamine (100 uL) and NH4Cl (50 mg). The reaction was purified by HPLC to give 23 mg of 2-(4-(1-(4-fluorophenyl)-1H-indazol-5-yl)tetrahydro-2H-pyran-4-yl)-2-methylpropanamide. (M+H)+=382.

1. extractionthe reaction was extracted from NaHCO3 with EtOAc×3
2. dry with materialThe combined organic layers were dried over MgSO4
3. filtrationfiltered
4. concentrationconcentrated
5. additiontreated with triethylamine (100 uL) and NH4Cl (50 mg)
6. customThe reaction was purified by HPLC