Potassium Phosphate, Tribasic → 2-(4-(dimethoxymethyl)pyridin-3-yl)-7-(trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one

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Reaction Steps

Using analogous conditions as described for the preparation of Example 1A above, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-4-d: 505.4 mg, 2.3503 mmol) was reacted with 3-Bromo-4-dimethoxymethyl-pyridine (I-52a: 600 mg, 2.5854 mmol), 1,4-dioxane (20 mL), copper iodide (44.6 mg, 0.2348 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (80.9 mg, 0.7052 mmol) and potassium phosphate (1.49 g, 7.0507 mmol) to afford the crude product. Purification by column chromatography on silica gel (1% methanol in CHCl3) afforded 850 mg of the product (98.8% yield).

Provenance & Evidence