反应详情

温度

-60 °C

In analogy with Example 1h), 5.0 g (16.37 mmol) of 5(S)-[1(S)-(Boc-amino)-2-phenylethyl]dihydrofuran-2-(3H)-one [Example 2b)] dissolved in 75 ml of THF are deprotonated, at -75° C., with 32.7 ml of a 1M solution of lithium bis(trimethylsilyl)amide in THF, and alkylated with 2.1 ml (18.0 mmol) of o-fluorobenzyl bromide (Fluka; Buchs/Switzerland) at -75° C. initially (heating to a maximum of -60° C. over a period of 60 min). Column chromatography (SiO2, hexane/ethyl acetate, 3:1) affords the title compound: TLC Rf (D)=0.61.