Potassium Phosphate, Tribasic → 2-(5-Fluoro-pyridin-3-yl)-7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one

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Reaction Steps

Using analogous reaction conditions as described in Example 1, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-16c: 90 mg, 0.419 mmol) was reacted with 3-bromo-5-fluoro-pyridine (73.67 mg, 0.419 mmol), 1,4-dioxane (10 mL), copper iodide (7.98 mg, 0.0419 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (17.85 mg, 0.126 mmol) and potassium phosphate (222 mg, 1.048 mmol) to afford the crude product. Purification by column chromatography on silica gel (0.5% methanol in DCM) afforded 35 mg of the product (27.19% yield).

Provenance & Evidence