反应详情

Methanesulfonic acid 1-(6-methoxy-[1,5]naphthyridin-4-yl)-pyrrolidin-3-yl ester (1.96 g, 6.1 mmol) was heated to 100° C. in ethylene diamine (10 mL, 150 mmol) overnight. The reaction mixture was cooled, diluted with water and extracted 4× with a solution of 10% isopropanol in chloroform. The combined organic layers were washed with brine, dried over magnesium sulfate, and purified by column chromatography (silica, 10% MeOH in chloroform) to afford the title coompound as a white solid (1.3 g, quantitative yield as an adduct of two moles of water): LC/MS m/z 288 (M+H)+.

1. temperatureThe reaction mixture was cooled
2. extractionextracted 4× with a solution of 10% isopropanol in chloroform
3. washThe combined organic layers were washed with brine
4. dry with materialdried over magnesium sulfate
5. custompurified by column chromatography (silica, 10% MeOH in chloroform)