Dimethylformamide → (5,8-Dihydro-6H-[1,7]naphthyridin-7-yl)-acetic acid tert-butyl ester

Participants

Reaction Steps

A DMF solution (8 mL) of 5,6,7,8-Tetrahydro-[1,7]naphthyridinehydrochloride (Preparation 233, 400 mg, 1.93 mmol), bromo-acetic acid tert-butyl ester (414.1 mg, 2.12 mmol) and triethylamine (1.64 mL, 11.92 mmol) was heated at 80° C. for 16 hours. The reaction mixture was diluted with EtOAc (40 mL), washed with water (3×25 mL), brine (20 mL), dried over Na2SO4 and evaporated to dryness in vacuo to afford the title compound as colorless sticky solid in 100% yield, 480 mg.

Provenance & Evidence