反应详情

温度

0 °C

To a solution containing Boc-N(Me)Ala-OH (76 mg, 0.37 mmol) in anhydrous NMP (4 mL) was cooled to 0° C. HATU (141 mg, 0.37 mmol) and DIPEA (148 mg, 1.14 mmol) were added followed by the addition of crude 51 (172 mg, 0.39 mmol) in anhydrous NMP (5 mL). The reaction mixture was slowly warmed to ambient temperature. After 16 h, the reaction mixture was diluted with EtOAc and washed successively with 1M HCl, aqueous NaHCO3, and brine, dried over anhydrous Na2SO4, filtered, and concentrated to afford 255 mg of crude 52 as an off-white-colored foam which was used without further purification. Mass spectrum, m/z [628.5] (M+H)+.

1. temperatureThe reaction mixture was slowly warmed to ambient temperature
2. washwashed successively with 1M HCl, aqueous NaHCO3, and brine
3. dry with materialdried over anhydrous Na2SO4
4. filtrationfiltered
5. concentrationconcentrated