Cesium carbonate → HCID 77845847, compound

Participants

Reaction Conditions

Reaction Steps

A solution of 5-(6-(4-fluoro-1H-indol-2-yl)-5-vinylpyrazin-2-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (50 mg, 0.08 mmol) in HCl/1,4-dioxane (1 mL) was stirred at 80° C. for 1 h under nitrogen atmosphere. The reaction mixture was concentrated; then the residue was used to the next step reaction without purification. To the residue in DMF, Cs2CO3 was added (53 mg, 0.16 mmol), the reaction mixture was stirred at 80° C. for 1 h under nitrogen atmosphere, concentrated and purified by prep-TLC (PE:EA=1:2) to give the desired product (10 mg, yield: 20%). 1H-NMR (CDCl3, 400 MHz) δ 8.56 (s, 1H), 8.03 (s, 1H), 7.90 (dd, J=9.2 Hz, 5.2 Hz, 2H), 7.64 (s, 1H), 7.29 (s, 1H), 7.09˜7.17 (m, 4H), 6.74˜6.78 (m, 1H), 5.85 (br s, 1H), 4.41 (t, J=6.8 Hz, 2H), 3.47 (t, J=6.8 Hz, 2H), 3.34 (s, 3H), 2.94 (d, J=4.8 Hz, 3H), 2.73 (s, 3H). MS (M+H)+: 614.

Provenance & Evidence