反应详情

To a solution of 300 mg (0.5 mmol) of 4-[4-((2S)-2-benzyloxycarbonylamino-2-tert-butoxycarbonyl-ethylamino)-2-methyl-pyrrolo[2,3-d]pyrimidin-7-yl]-butyric acid ethyl ester (example 2b) in 5 ml of absol. THF were added 124 mg (1.82 mmol) of sodium ethanolate and 155 mg (1.56 mmol) of 1,4,5,6-tetrahydro-2-aminopyrimidine and the solution was stirred at room temperature for 6 hours. The mixture was brought to pH 7.0 and the solvent was removed in vacuo. The residue was chromatographed on silica gel eluting with DCM/MeOH/AcOH/H2O (90:10:1:1). Yield: 28 mg.

1. customthe solvent was removed in vacuo
2. customThe residue was chromatographed on silica gel eluting with DCM/MeOH/AcOH/H2O (90:10:1:1)