反应详情

The objective compound was prepared by the same procedure for the intermediate 1, using a 2-(4-benzyloxy-phenyl)-propionic acid (2.70 g, 10.5 mmol), PCl5 (2.30 g, 10.5 mmol), and 2-amino-4,6-dichloro-benzoic acid methyl ester (1.54 g, 7.0 mmol). After normal workup, the pure objective compound (2.90 g, 91%) was obtained as white solid by a flash column chromatography (n-hexane:EtOAc=10:1): 1H NMR (200 MHz, CDCl3) δ 1.59 (d, J=7.0 Hz, 3H, CH3), 3.65-3.76 (m, 1H, CH), 3.76 (s, 3H, CO2CH3), 5.09 (s, 2H, OCH2Ph), 6.93-6.97 (m, 3H, ArH), 7.14 (d, J=1.8 Hz, 1H, ArH), 7.26-7.48 (m, 6H, ArH), 8.42 (d, J=1.8 Hz, 1H, ArH), 9.02 (s, 1H, NH); MS(EI) m/e 458 [M+], 426, 336, 301, 121, 91.