Tetrahydrofuran → (S)-2-Amino-1-{4-[(4-benzyloxy-phenyl)-(3-methyl-but-2-enyl)-amino]-piperidin-1-yl}-4-methyl-pentan-1-one

Participants

Reaction Conditions

Reaction Steps

4-(4-Benzyloxy-phenylamino)-piperidine-1-carboxylic acid tert-butyl ester (5.0 g, 13.1 mmol) was dissolved in THF (65 mL), then treated with N,N-diisopropylethylamine (9.1 mL, 52.4 mmol) and 4-bromo-2-methyl-2-butene (3.0 mL, 26.2 mmol). The reaction was heated to 40° C. for 18 hours, then concentrated in vacuo. The residue was chromatographed on silica gel eluting with 5:1 hexane/EtOAc to give 5.15 g (87%) of the desired compound.

Provenance & Evidence