反应详情

Analogously to Example 21 D) 1)c), 1.13 g (3.70 mmol) of 5(S)-[1(S)-(Boc-amino)-2-phenylethyl]-dihydrofuran-2-(3H)-one [Example 21 D) 1)b)] dissolved in 4.8 ml of THF and 0.75 ml of 1,3-dimethyl-3,4,5,6-tetrahydro-2(1H)-pyrimidinone are deprotonated at -75° C. with 7.25 ml of lithium bis(trimethylsilyl)amide 1M in THF, and alkylated (15 min) with 1.2 g (3.7 mmol) of p-benzyloxybenzyl iodide in 2 ml of THF. Column chromatography (SiO2, hexane/ethyl acetate 2:1) yields the pure title compound: TLC Rf (D)=0.30; tRet (II)=28.2 min; FAB-MS (M+H)+ =502.

1. customalkylated (15 min)