Trifluoroacetic acid → Methyl (2S)-2-amino-3-[4-(1,1-dioxido-3-oxoisothiazolidin-5-yl)-3-fluorophenyl]-propanoate trifluoroacetate

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Reaction Steps

Methyl (2S)-2-[(tert-butoxycarbonyl)amino]-3-[4-(2-tert-butyl-1,1-dioxido-3-oxo-isothiazolidin-5-yl)-3-fluorophenyl]propanoate (1.10 g, 2.26 mmol) in trifluoroacetic acid (10.0 mL) was heated for 2 minutes at 130° C. in the microwave. The solution was concentrated in vacuo and purified by preparative LCMS to afford product as a white solid (614 mg, 61%). 1H NMR (400 MHz, CD3OD): δ 7.53 (m, 1H), 7.18–7.14 (m, 2H), 5.33–5.30 (m, 1H), 4.39 (m, 1H), 3.82 (s, 3H), 3.43–3.12 (m, 4H). LCMS found for C13H16FN2O5S (M+H)+: m/z=331.

Provenance & Evidence