Trifluoroacetic acid → HCID 136121356, compound

Participants

Reaction Steps

To a solution of tert-butyl (R)-1-(6-fluoro-2-(2-hydroxyphenyl)quinazolin-4-yl)pyrrolidin-3-ylcarbamate (480 mg, 1.11 mmol) in CH2Cl2 (10 mL) was added TFA (4 mL). The reaction was stirred for an hour, diluted with 10 mL CH2Cl2, and neutralized with a saturated aqueous NaHCO3 solution. The aqueous layer was extracted twice with CH2Cl2. The combined organic layers were dried over MgSO4, filtered, and concentrated. Purification via silica gel chromatography using 3-20% EtOAc/CH2Cl2 gave 2-(4-((R)-3-aminopyrrolidin-1-yl)-6-fluoroquinazolin-2-yl)phenol. LC/MS: m/z 325.5 (M+H)+ at 1.26 min (10%-99% CH3CN (0.035% TFA)/H2O (0.05% TFA)).

Provenance & Evidence