1,2,3,4-Tetrahydroisoquinoline → 2-(4,6-Dimethoxy-5-nitropyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinoline

Participants

Reaction Steps

1,8-diazabicyclo[5.4.0]undec-7-ene (0.304 g, 2 mmol) was added to a mixture of 4a (0.438 g, 2 mmol) and 1,2,3,4-tetrahydroisoquinoline (0.293 g, 2.2 mmol) in DMF (3 ml) at 0° C. over 5 minutes. The mixture was stirred for an additional 5 minutes at room temperature. The mixture was washed with brine, extracted with ethyl acetate and chromatographed to yield 4b (0.592 g, 1.87 mmol, 94%).

Provenance & Evidence