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

関与物質

反応手順

Using analogous reaction conditions as described in Example 1, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-4-d: 120 mg, 0.558 mmol) was reacted with 3-iodo-4-methyl-pyridine (134 mg, 0.613 mmol), 1,4-dioxane (5 mL), copper iodide (10.6 mg, 0.0558 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (23.7 mg, 0.167 mmol) and potassium phosphate (354 mg, 1.674 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% methanol in CHCl3), followed by preparative HPLC afforded 20 mg of the product (11.71% yield).

情報源と証拠