反应详情

Following the procedure as described in Example 24, except using the material from Example 68 (254 mg, 0.984 mmol), N-alpha-t-BOC-L-Alanine (201 mg, 1.06 mmol), 1-hydroxy-7-azabenzotriazole (70.0 mg, 0.514 mmol), CH2Cl2 (15 mL), N-methylmorpholine (224 μlit, 2.04 mmol), and EDC (229 mg, 1.21 mmol), and stirring at room temp for 45 min., 267.3 mg (76%) of the title compound is obtained as a yellow solid. Purification is done by BIOTAGE® Silica gel chromatography on a 25 g Thompson Single Step silica cartridge using a linear gradient from 100% CH2Cl2 to 100% EtOAc, over 8.5 column volumes, with a hold at 100% EtOAc for 15 column volumes. LC/MS (Condition A): ret. T=2.54 min, (M+H)+ 357.20.