Trifluoroacetic acid → 1-{1-[(R)-2-amino-3-(4-methoxyphenyl)propionyl]-4-cyclohexylpiperidin-4-yl}butan-1-one

Participants

Reaction Steps

1.4 g (2.7 mmol) of tert-butyl[(R)-2-(4-butyryl-4-cyclohexylpiperidin-1-yl)-1-(4-methoxybenzyl)-2-oxoethyl]carbamate are placed in a mixture composed of 40 mL of DCM and 8 mL of trifluoroacetic acid. The reaction medium is stirred for 2 hours at room temperature and the reaction is then stopped by adding aqueous 1N sodium hydroxide solution. After extracting with dichloromethane, the organic phase is dried over sodium sulfate and then filtered and concentrated. 1.24 g of 1-{1-[(R)-2-amino-3-(4-methoxyphenyl)propionyl]-4-cyclohexylpiperidin-4-yl}butan-1-one in the form of a colourless oil are obtained in a yield of 100%.

Provenance & Evidence