Triethylamine → 4-Piperidineacetic acid

Participants

Reaction Steps

A mixture of intermediate (24) (0.000084 mol), PyBOP (0.00017 mol) and triethylamine (0.5 ml) in DCM (5 ml) was stirred for 60 minutes at room temperature. Methyl hydroxyacetate (0.0001 mol) was added and the reaction mixture was stirred for 3 hours at 40° C., then over the weekend at room temperature. Water (2 ml) was added. The mixture was stirred for 15 minutes, then filtered through Extrelut™ and the organic filtrate was evaporated. The residue was purified by HPLC. The product fractions were collected and the solvent was evaporated, yielding 4-piperidineacetic acid, α-phenyl-1-[4-[[[4′-(trifluoromethyl)[1,1′-biphenyl]-2-yl]carbonyl]amino]-phenyl]-, 2-methoxy-2-oxoethyl ester (compound 20).

Provenance & Evidence