Diisopropylethylamine → 1-{2-[4-(4-Hydroxy-4-methyl-piperidin-1-ylmethyl)-phenyl]-ethyl}-4-(pyridin-2-ylmethoxy)-1H-pyridin-2-one

Participants

Reaction Steps

To 140 mg (0.26 mmol) 1-[2-(4-bromomethyl-phenyl)-ethyl]-4-(pyridin-2-ylmethoxy)-1H-pyridin-2-one (example 3.3a) in 1.5 mL DMF is added 61 mg (0.53 mmol) 4-hydroxy-4-methylpiperidine and 0.12 mL (0.66 mmol) N-ethyl-diisopropylamine at RT. The reaction mixture is stirred 2 h at RT and is directly transferred to a reverse HPLC for purification (Waters symmetry, C18; water (0.15% formic acid)/acetonitrile 95:5 to 10:90).

Provenance & Evidence