反应详情

2′-Methyl-5′-[(2-pyrrolidin-1-ylisonicotinoyl)amino]-1,1′-biphenyl-4-carboxylic acid 5′-[(2-Chloroisonicotinoyl)amino]-2′-methyl-1,1′-biphenyl-4-carboxylic acid (600 mg, 1.64 mmol) and pyrrolidine (0.6 ml) were heated in a sealed tube at 90° C. for 5 h. The excess pyrrolidine was evaporated under vacuum and the residue purified by flash chromatography (silica) eluting with DCM/ethanol/ammonia (20:8:1). The solvents were evaporated under vacuum to give 2′-methyl-5′-[(2-pyrrolidin-1-ylisonicotinoyl)amino]-1,1′-biphenyl-4-carboxylic acid (546 mg, 83%). LCMS: retention time 2.74 min, MH+402.

1. customThe excess pyrrolidine was evaporated under vacuum
2. customthe residue purified by flash chromatography (silica)
3. washeluting with DCM/ethanol/ammonia (20:8:1)
4. customThe solvents were evaporated under vacuum