Formic Acid → tert-Butyl (4-Cyano-2-(methylsulfonyl)phenyl)(phenylsulfonyl)methylcarbamate

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Reaction Steps

Formic acid (6.2 mL, 164 mmol) is added to a mixture of tert-butyl carbamate (3.05 g, 26.0 mmol), 4-formyl-3-(methylsulfonyl)benzonitrile (5.44 g, 26.0 mmol, preparation according to WO09080199) and sodium benzenesulfinate (4.27 g, 26.0 mmol) in THF (10.0 mL) and water (25.0 mL) and the reaction mixture is stirred at room temperature for 4 days. Water (30 mL) is added and the precipitate is filtered off, washed with water and acetonitrile and dried. Yield: 5.10 g. ESI mass spectrum: [M+H]+=451; Retention time HPLC: 0.59 min (X012_S01).

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