反应详情

According to the procedure of Preparation 4(c), except using tert-butyl 4-fluoro-3-[(phenethylamino)methyl]benzoate (5.00 g, 15.2 mmole), N-(benzyloxycarbonyl)-D-serine (3.83 g, 16 mmole), HOBt.H2O (2.16 g, 16 mmole), Et3N (2.24 mL, 16 mmole), EDC.HCl (3.07 g, 16 mmole), and 1:1 DMF/CH2Cl2 (75 mL), the title compound (3.44 g, 41%) was prepared as a thick oil following flash chromatography on silica gel (40% EtOAc/hexanes): 1H NMR (300 MHz, DMSO-d6) mixture of amide rotamers δ 7.31-8.18 (m, 2 H), 7.19-7.29 (m, 11 H), 4.86-5.11 (m, 4 H), 4.33-4.79 (m, 3 H), 3.49-3.80 (m, 4 H), 1.51 (s, 9 H).