反应详情

Using analogous conditions as described for the preparation of Example 1A above, 7-(trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one (I-4-d: 100 mg, 0.465 mmol) was reacted with 3-bromo-4-(pyrrolidin-1-ylmethyl)pyridine (I-52a: 140 mg, 0.558 mmol), 1,4-dioxane (10 mL), copper iodide (8.8 mg, 0.0465 mmol), trans-N,N′-dimethyl-cyclohexyl-1, 2-diamine (19.8 mg, 0.139 mmol) and potassium phosphate (295 mg, 1.395 mmol) to afford the crude product. Purification by column chromatography on silica gel (12% methanol in CHCl3), followed by preparative HPLC afforded 7 mg of the product (4.02% yield).

1. customas described for the preparation of Example 1A above
2. customto afford the crude product
3. customPurification by column chromatography on silica gel (12% methanol in CHCl3)