1-Ethoxycarbonyl-4-(4-fluoro-2-nitroanilino)piperidine → 4-(2-Amino-4-fluoro-phenylamino)-piperidine-1-carboxylic acid ethyl ester

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Reaction Steps

This 1-ethoxycarbonyl-4-(4-fluoro-2-nitroanilino)piperidine (5.7 g, 18.3 mmol.) was dissolved in THF (50 mL) and diluted with ethanol (100 mL). After addition of 5% platinum/carbon catalyst (1.2 g), the hydrogenation of the nitro functional group was carried out at atmospheric pressure via a balloon over a four hour period. The catalyst was removed and the solvents evaporated to give 1-ethoxycarbonyl-4-(2-amino-4-fluoroanilino)-piperidine as a viscous oil which was used as is.

Provenance & Evidence