反应详情

To a solution of 4-{[(4,4-dimethyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indol-7-yl)carbonyl]amino}-1-methyl-1H-imidazole-2-carboxylic acid (104 mg, 0.27 mmol) in DMF (2 mL) are added N-hydroxybenzotriazole (74 mg, 0.55 mmol) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (105 mg, 0.55 mmol). After stifling for 10 min at 50° C., tert-butylamine (0.06 mL, 0.55 mmol), N,N-diisopropylethylamine (0.10 mL, 0.55 mmol) and 4-dimethylaminopyridine (6.7 mg, 0.06 mmol) are added. The reaction mixture is stirred at room temperature for 8 h. The solvent is removed under N2 stream to afford the crude compound which is purified by flash column chromatography to afford the title compound (61 mg, 51%). LCMS (ESMS): m/z 437.78 (M+H+).

1. customThe solvent is removed under N2 stream
2. customto afford the crude compound which
3. customis purified by flash column chromatography