反应详情

A mixture of 2-amino-nicotinic acid ethyl ester (13.845 g), ClCH2CHO (58 mL), and NaHCO3 (11.85 g) was stirred in EtOH (500 mL) at reflux overnight. The reaction mixture was concentrated, diluted with H2O, and extracted with DCM. The product was purified by ISCO using 100% EtOAc first (to remove unreacted starting material), then using 100% DCM to 5% MeOH/DCM. The product eluted at 3% MeOH/DCM, providing imidazo[1,2-a]pyridine-8-carboxylic acid ethyl ester (10.5 g).

1. temperatureat reflux overnight
2. concentrationThe reaction mixture was concentrated
3. additiondiluted with H2O
4. extractionextracted with DCM
5. customThe product was purified by ISCO
6. custom100% EtOAc first (to remove unreacted starting material)
7. washThe product eluted at 3% MeOH/DCM