反应详情

Diethylamine(1.2 mmol) and 2-[(5-chloro-1H-indol-2-carbonyl)-amino]3-phenyl-propionic acid (0.6 mmol) were coupled according to procedure A (0-25° C. for 5 days) substituting the following workup: the crude product was suspended in 1:1 chloroform/dichloromethane, sonicated, filtered to remove solids, concentrated, and the residue purified by column chromatography on silica gel eluted with 10, 20 and 30% ethyl acetate in hexanes: Yield 14 mg, 6%; HPLC (60/40) 8.88 minutes (98%); PBMS 398/400 (MH+, 100%);

1. customwere coupled according to procedure A (0-25° C. for 5 days)
2. customsonicated
3. filtrationfiltered
4. customto remove solids
5. concentrationconcentrated
6. customthe residue purified by column chromatography on silica gel
7. washeluted with 10, 20 and 30% ethyl acetate in hexanes
8. customHPLC (60/40) 8.88 minutes (98%)