Benzoic acid, 3-amino-, methyl ester → 4-[(5-Chloro-2-fluoro-benzyl)-(3-methoxycarbonyl-phenyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester

Participants

Reaction Steps

Using general procedure A with methyl 3-aminobenzoate (2.16 g, 14.3 mmol) and 1-Boc-4-piperidone (2.39 g, 12.0 mmol) followed by general procedure H with the resulting amine and 5-chloro-2-fluorobenzyl bromide (65%, 1.04 g, 3.0 mmol) gave 4-[(5-chloro-2-fluoro-benzyl)-(3-methoxycarbonyl-phenyl)-amino]-piperidine-1-carboxylic acid tert-butyl ester as a white foam (911 mg, 47% over 2 steps).

Provenance & Evidence