反应详情

(S)-tert-butyl 2-(7-(6-(2-((S)-1-((S)-2-(methoxycarbonylamino)-3-methylbutanoyl)pyrrolidin-2-yl)-1H-imidazol-5-yl)naphthalen-2-yl)-4,5-dihydro-1H-naphtho[1,2-d]imidazol-2-yl)pyrrolidine-1-carboxylate (246 mg, 0.325 mmol) was dissolved in dichloromethane (10 mL) and HCl (4 M in dioxane, 2 mL) was added. After stirring at RT for 1 h 40 min, the reaction mixture was concentrated. The crude residue was treated with (R)-2-(methoxycarbonylamino)-2-phenylacetic acid (75 mg, 0.358 mmol), COMU (139 mg, 0.325 mmol) and DMF (6 mL). DIPEA was added to the stirred reaction mixture dropwise. After 35 min, 1 mL H2O was added and the crude solution was purified by HPLC to afford the title compound (177 mg, 64%). MS (ESI) m/z 849 [M+H]+.

1. concentrationthe reaction mixture was concentrated
2. waitAfter 35 min
3. customthe crude solution was purified by HPLC