Ethyl orthoformate → [2,5-difluoro-4-(1H-tetrazol-1-yl)phenyl]acetic acid

Participants

Reaction Conditions

Reaction Steps

A solution of (4-amino-2,5-difluorophenyl)acetic acid (380 mg, 2.0 mmol) and triethyl orthoformate (902 mg, 6.1 mmol) in HOAc (10 mL) was added sodium azide (158 mg, 2.44 mmol) and the mixture was heated to 100° C. for 3 hours. After the reaction was completed, the reaction mixture was cooled to ambient temperature. The solvent was removed under vacuum. The residue was dissolved in EtOAc, washed with water, dried over anhydrous sodium sulfate, and concentrated. The [2,5-difluoro-4-(1H-tetrazol-1-yl)phenyl]acetic acid was directly used in next step.

Provenance & Evidence