反应详情

A solution of isoxazole 5-carboxylic acid (2.81 g), N-methoxy-N-methylamine hydrochloride (2.49 g), EDCI (4.96 g), dimethylaminopyridine (3.15 g) and 4-methylmorpholine (2.8 ml) in dichloromethane (20 ml) was stirred for 18 h. 2M Hydrochloric acid was added and the mixture was extracted with dichloromethane (three times). The organic layers were washed with aqueous sodium hydrogen carbonate and then brine, combined, dried (magnesium sulphate), evaporated and purified by chromatography on silica eluting with petrol-ether to give the sub-title compound as a colourless oil (2.94 g, 76%).

1. extractionthe mixture was extracted with dichloromethane (three times)
2. washThe organic layers were washed with aqueous sodium hydrogen carbonate
3. dry with materialdried (magnesium sulphate)
4. customevaporated
5. custompurified by chromatography on silica eluting with petrol-ether