反应详情

A solution of 2-cyclopropyl-4-methyl-6-morpholin-4-yl-pyridine-3-carboxylic acid ethyl ester (16.8 g, 57.8 mmol) in methanol-tetrahydrofuran (1:1) (90 ml) is treated for 3 days with a 2M aqueous solution of sodium hydroxide at reflux. The organic solvent is distilled off and the aqueous layer treated with 2M hydrochloric acid, and extracted with ethyl acetate. The combined organic layers are dried over magnesium sulphate and evaporated to dryness. The crude product is purified by flash chromatography (silica gel, 75% ethyl acetate/cyclohexane) to yield 2-cyclopropyl-4-methyl-6-morpholin-4-yl-pyridine-3-carboxylic acid (10.4 g, 39.6 mmol, 69%).

1. temperatureat reflux
2. distillationThe organic solvent is distilled off
3. additionthe aqueous layer treated with 2M hydrochloric acid
4. extractionextracted with ethyl acetate
5. dry with materialThe combined organic layers are dried over magnesium sulphate
6. customevaporated to dryness
7. customThe crude product is purified by flash chromatography (silica gel, 75% ethyl acetate/cyclohexane)