Morpholine → 2-Methyl-1-morpholin-4-yl-2-[5-(5,6,7,8-tetrahydro-[1,8]naphthyridin-3-yl)-pyridin-3-yl]-propan-1-one

Participants

Reaction Steps

To a suspension 6-[5-(1-carboxy-1-methyl-ethyl)-pyridin-3-yl]-3,4-dihydro-2H-[1,8]naphthyridine-1-carboxylic acid tert-butyl ester (50 mg, 0.13 mmol) in DMF (1 mL) is added HATU (57 mg, 0.15 mmol), morpholine (11 mg, 0.13 mmol) and N,N-diisopropylethylamine (0.14 mL, 0.81 mmol). The mixture is stirred at room temperature for 16 h. The reaction mixture is purified by reverse phase HPLC (mobile phase contains 1% TFA) to afford 53 mg of 2-methyl-1-morpholin-4-yl-2-[5-(5,6,7,8-tetrahydro-[1,8]naphthyridin-3-yl)-pyridin-3-yl]-propan-1-one.

Provenance & Evidence