Acetic Acid → HCID 57863420, compound

Participants

Reaction Steps

Combine 2-(4-{7-[4-(2-Amino-ethanesulfonyl)-phenyl]-imidazo[1,2-a]pyridin-3-yl}-phenyl)-N-(5-tert-butyl-isoxazol-3-yl)-acetamide (0.87 g, 1.38 mmol) with acetic acid (1 mL), methanol (20 mL) and acetaldehyde (0.152 g, 3.45 mmol) at ambient temperature under nitrogen for 10 minutes. Add sodium cyanoborohydride at ambient temperature. The reaction is complete within 3 hours. Evaporate under vacuum, re-dissolved in methanol and dichloromethane and load onto an SCX column. Wash the column with dichloromethane (50 mL) and methanol (50 mL) and elute with methanolic ammonia. Chromatography on silica (0→2→4→5%) methanol and dichloromethane gives the title compound (21.0 mg). MS(ES), m/z 614 (M+1).

Provenance & Evidence