反应详情

1-Piperazinecarboxylic acid t-butyl ester (1.2 mmol) and 2-[(5-chloro-1H-indole-2-carbonyl)-amino]-3-phenyl-propionic acid (0.6 mmol) were coupled according to procedure A (0-25° C. reaction temperature, reaction time 4 days, extraction with acid first, then base), and the crude product purified by column chromatography on silica gel eluted with 30% ethyl acetate in hexanes to give a colorless foam: Yield 290 mg, 95%; HPLC (70/30) 6.23 min (99%); PBMS 512/514 (MH+, 100%);

1. custom0-25° C. reaction temperature, reaction time 4 days, extraction with acid first
2. custombase), and the crude product purified by column chromatography on silica gel
3. washeluted with 30% ethyl acetate in hexanes
4. customto give a colorless foam