Trifluoroacetic acid → [2-(4-fluoro-3-methoxyphenyl)-4-oxo-6-(3,6,6-trimethylperhydro-1,4-diazepin-1-yl)-4H-quinazolin-3-yl]acetic acid

Participants

Reaction Steps

[2-(4-Fluoro-3-methoxyphenyl)-4-oxo-6-(3,6,6-trimethylperhydro-1,4-diazepin-1-yl)-4H-quinazolin-3-yl]acetic acid tert-butyl ester (INTERMEDIATE VII.12) (160 mg, 0.305 mmol) was dissolved in DCM (10 mL) and TFA (3 mL) added. The reaction mixture was stirred at room temperature overnight. Crude reaction mixture was poured directly onto an SCX cartridge, the cartridge was washed with MeOH and product eluted with 2N NH3/MeOH. Solvent was removed under reduced pressure to afford [2-(4-fluoro-3-methoxyphenyl)-4-oxo-6-(3,6,6-trimethylperhydro-1,4-diazepin-1-yl)-4H-quinazolin-3-yl]acetic acid (INTERMEDIATE IX.1) which was used without further purification.

Provenance & Evidence