反应详情

温度

75 °C

Lithium borohydride (0.1 g, 4.92 mmol, 1.8 eq) is added to a solution of methyl 1-{4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl}-5-oxopyrrolidine-3-carboxylate a54 (0.99 g, 2.73 mmol, 1 eq) in tetrahydrofuran (20 ml) and methanol (0.35 ml). The mixture is stirred at 75° C. for 1 h, then cooled to 0° C. and a solution of 1 M hydrochloric acid is added. A solution of 2M sodium hydroxide is then added to reach a pH of 10. The aqueous layer is extracted twice with ethyl acetate, then the organic layers are dried over magnesium sulfate, and concentrated under vacuum to give 0.79 g of 4-(hydroxymethyl)-1-{4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl}pyrrolidin-2-one 72 as a colorless oil.

1. temperaturecooled to 0° C.
2. extractionThe aqueous layer is extracted twice with ethyl acetate
3. dry with materialthe organic layers are dried over magnesium sulfate
4. concentrationconcentrated under vacuum