反应详情

A mixture of 6-[2-(methoxymethyl)pyrrolidin-1-yl]-5-methylnicotinonitrile (591 mg; 2.56 mmol; 1 eq.) and potassium hydroxide (717 mg; 12.8 mmol; 5 eq.) in water (20 mL) was stirred at reflux for 16 hours. The pH was adjusted to 5-6 with HCl 1M and the aqueous layer extracted with EtOAc. The combined organic phase was dried over MgSO4 and concentrated in vacuo to afford the title compound as a white solid (0.63 g, 99%). LC/MS: 219.1 (M+H)+. HPLC (Method A): Rt 1.44 min (purity 96.6%).

1. temperatureat reflux for 16 hours
2. extractionthe aqueous layer extracted with EtOAc
3. dry with materialThe combined organic phase was dried over MgSO4
4. concentrationconcentrated in vacuo