Potassium Phosphate, Tribasic → 8-fluoro-7-(trifluoromethyl)-2-(4-(trifluoromethyl)pyridin-3-yl)-3,4-dihydroisoquinolin-1(2H)-one

Participants

Reaction Steps

8-Fluoro-7-(trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one (I-77d: 100 mg, 0.4288 mmol) was reacted with 3-bromo-4-(trifluoromethyl)-pyridine (120 mg, 0.5575 mmol), 1,4-dioxane (5 mL), copper iodide (8.1 mg, 0.0428 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (6.1 mg, 0.0428 mmol) and potassium phosphate (273 mg, 1.2866 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% methanol in CHCl3), followed by preparative HPLC afforded 25 mg of the product (15.4% yield).

Provenance & Evidence