反应详情

温度

65 °C

To a degassed solution of 2-[(4-Iodo-benzyl)-(4-methoxy-2,3,6-trimethyl-benzenesulfonyl)-amino]-3-phenyl-propionic acid methyl ester (40 mg, 0.068 mmol) and benzofuran-2-boronic acid (20 mg, 0.124 mmol) in a mixture of DME (3 mL) and 2M aqueous Na2CO3 (1.5 mL), Pd(PPh3)4 (4 mg) was added and the reaction mixture was stirred at 65° C. for 2 h under a N2 atmosphere. The reaction mixture was diluted with ethyl acetate and water. The organic layer was separated, dried (Na2SO4), concentrated. The residue was purified by column chromatography using ethyl acetate and hexane (1:9) to obtain 2-[(4-Benzofuran-2-yl-benzyl)-(4-methoxy-2,3,6-trimethyl-benzenesulfonyl)-amino]-3-phenyl-propionic acid methyl ester (39 mg, 100%) as a thick syrup. 1H NMR (af-2783) (CDCl3, 400 MHz): δ7.2 (d, 2H), 7.62 (d, 1H), 7.55 (d, 1H), 7.30-7.15 (m, 7H), 7.12 (d, 2H), 6.96 (s, 1H), 6.51 (s, 1H), 4.72 (m, 3H), 3.80, 3.40 (2s, 6H), 3.28 (dd, 1H), 3.02 (dd, 1H), 2.71, 2.58, 2.12 (3s, 9H).

1. additionwas added
2. customThe organic layer was separated
3. dry with materialdried (Na2SO4)
4. concentrationconcentrated
5. customThe residue was purified by column chromatography