Trifluoroacetic acid → (3R,6S)-3-Amino-6-(2,3-difluorophenyl)azepane-2-thione

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Reaction Steps

Trifluoroacetic acid (5 mL, 49.6 mmol) was added to a solution of tert-butyl (3R,6S)-6-(2,3-difluorophenyl)-2-thioxoazepan-3-ylcarbamate (680 mg, 1.91 mmol) in dichloromethane (10 mL). After 1 h, the reaction was concentrated. Saturated aqueous sodium bicarbonate was added and the mixture was extracted with dichloromethane (3×). The combined organic extracts were dried over magnesium sulfate, filtered, and concentrated to give the title compound (489 g). MS 257.0 (M+1).

Provenance & Evidence