2,3-Dichloropyridine → 7-(3-Chloropyridin-2-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one

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Reaction Conditions

Reaction Steps

5,6,7,8-Tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one (600 mg, 4.0 mmol) was dissoled in a mixture of dioxane/N,N-dimethylacetamide (4:1) (2 mL). To the mixture was added 2,3-dichloropyridine (1.8 g, 12.0 mmol) and N,N-diisopropylethylamine (0.7 mL, 4.0 mmol). The mixture was heated at 150° C. in a microwave (Emrys Optimizer model, Personal Chemistry) for 16 h. The solvents were removed under vacuum and the residue was dissolved in ethyl acetate and washed with sat. NaHCO3 and brine. The organic layer was dried over Na2SO4, filtered and evaporated to give a yellow solid (900 mg, 86%), which was used as such for the next step.

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