反应详情

温度

60 °C

2.33 g (14.4 mmol) of 1-(3-chloropropyl)pyrrolidin-2-one [CAS Reg. No. 91152-30-6] and 4.69 g (14.4 mmol) of anhydrous cesium carbonate are added to a solution of 3.2 g (7.2 mmol) of methyl 4-{(4E)-5-(2-hydroxyphenyl)-3-[4-(methoxycarbonyl)benzyl]pent-4-en-1-yl}benzoate (enantiomer 1, Example 19A) in 50 ml of dry dioxane, and the mixture is then stirred at 60° C. for 12 h. The mixture is then filtered, and the filtrate is evaporated to dryness. The crude product obtained is purified by flash chromatography on silica gel (mobile phase: cyclohexane/ethyl acetate 10:1→2:1→1:1). This gives 2.98 g (5.23 mmol, 72% of theory) of a colorless oil.

1. filtrationThe mixture is then filtered
2. customthe filtrate is evaporated to dryness