2-Naphthylalanine → 1-{2-[1-(4-Fluoro-benzyl)-6,8-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-ethyl}-3-(2-methyl-quinolin-4-yl)-urea

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-(4-fluoro-benzyl)-6,8-dimethoxy-1,2,3,4-tetrahydro-isoquinoline (example A1, 50 mg, 0.16 mmol) in anhydrous THF (2.5 mL) is added 1-(2-chloro-ethyl)-3-(2-methyl-quinolin-4-yl)-urea (example D1, 43.8 mg, 0.16 mmol), TEA (34.6 μL, 0.25 mmol) and Nal (2.5 mg, 0.017 mmol). The mixture is stirred at 75° C. for five days in a sealed flask. The reaction mixture is evaporated, and the residue is purified by preparative HPLC to provide the title compound.

Provenance & Evidence