反应详情

To a suspension of 1.19 g (8.0 mmol) of 5-hydroxymethylimidazo[1,2-a]pyridine in 10 ml of dichloromethane, 4.05 ml (56 mmol) of thionyl chloride was added, followed by stirring at room temperature for 1 hour, after which the solvent was distilled off. To a solution of this residue and 0.94 g (8.0 mmol) of thiazolidine-2,4-dione in 15 ml of N,N-dimethylformamide, 2.40 ml (16.0 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added, followed by stirring at 80° C. for 16 hours. After the reaction mixture was cooled, water was added; the mixture was extracted with ethyl acetate and dried, after which the solvent was distilled off. The residue was purified by recrystallization (solvent, chloroform/ethyl acetate/diethyl ether) to yield 247 mg (12.5%, light brown powder) of the desired product.

1. additionwas added
2. distillationafter which the solvent was distilled off
3. stirringby stirring at 80° C. for 16 hours
4. temperatureAfter the reaction mixture was cooled
5. extractionthe mixture was extracted with ethyl acetate
6. customdried
7. distillationafter which the solvent was distilled off
8. customThe residue was purified by recrystallization (solvent, chloroform/ethyl acetate/diethyl ether)