反应详情

温度

100 °C

A suspension of 7-methoxy-2(1H)-quinolinone (405 mg; commercial) in DMF (10 mL) was treated with NaH (111 mg; 50% dispersion in oil). The mixture was stirred at rt for 30 min before the addition of a solution of 3-[[(methylsulfonyl)oxy]methyl]-1-azetidinecarboxylic acid tert-butyl ester (674 mg; prepared according to WO 02/066470) in DMF (2 mL). The mixture was heated at 100° C. overnight. The reaction mixture was partitioned between EA and water. The org. phase was dried over MgSO4, concentrated under reduced pressure and purified by CC (Hept/EA 2:1 to 0:1). The second eluting compound was isolated as a colourless foam (350 mg, 44% yield).

1. customThe reaction mixture was partitioned between EA and water
2. dry with materialphase was dried over MgSO4
3. concentrationconcentrated under reduced pressure
4. custompurified by CC (Hept/EA 2:1 to 0:1)