反应详情

To a solution of 7-amino-1-trifluoroacetyl-1,2,3,4-tetrahydroquinoline (D5) (1.17 g, 4.78 mmol) in DCM (20 ml) was added 4-biphenylcarboxylic acid (1.14 g, 5.73 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (1.06 g, 5.73 mmol) and 4-dimethylaminopyridine (70 mg, 0.57 mmol) and the reaction stirred at room temperature. After 3.75 h the reaction mixture was treated with 2M sodium hydroxide solution overnight. An acid/base work-up followed by flash column chromatography with an EtOAc/60-80° C. petroleum ether gradient gave the title compound as a beige solid. 1H NMR (250 MHz, CDCl3) δ (ppm): 7.91 (d, 2H), 7.63 (m, 5H), 7.47 (t, 2H), 7.41 (t, 1H), 7.11 (d, 1H), 6.91 (d, 1H), 6.61 (dd, 1H), 3.94 (br, 1H), 3.31 (m, 2H), 2.74 (t, 2H), 1.93 (m, 2H), 1.57 (br, 2H).