Ethanol → rac-tert-butyl N-[(1R,2S)-2-(4-aminophenyl)cyclopropyl]carbamate

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Reaction Steps

1.39 g (5.0 mmol) of the product prepared in step 15.2 are dissolved in 25 mL of hot ethyl acetate. After cooling to room temperature, 25 mL of absolute ethanol and 0.057 g (0.25 mmol) of platinum (IV) oxide are successively added. The reaction mixture is placed under a hydrogen pressure of 2.75 bar for 2 hours, and is filtered through thin glass fibre paper. The filtrate is concentrated under vacuum and purified by chromatography on a column of silica, eluting with a cyclohexane/ethyl acetate gradient (from 70/30 to 55/45). 1.05 g of the expected product are obtained. Yield=85%.

Provenance & Evidence