反应详情

Using analogous conditions and workup as described for the preparation of Compound 1A, 8-Fluoro-3,4-dihydro-2H-benzo[4,5]thieno[3,2-c]pyridin-1-one (I-50 g: 100 mg, 0.452 mmol) was reacted with 3-iodo-4-methylpyridine (99.09 mg, 0.452 mmol), 1,4-dioxane (5 mL), copper iodide (8.64 mg, 0.0452 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (19.25 mg, 0.1356 mmol) and potassium phosphate (287.44 mg, 1.356 mmol) at 115° C. overnight under nitrogen atmosphere to afford the crude product. Purification by column chromatography on silica gel (1.5% methanol in CHCl3) afforded 95 mg of the product (67.37% yield).

1. customto afford the crude product
2. customPurification by column chromatography on silica gel (1.5% methanol in CHCl3)