反应详情

To the crude (S)-2-(4-isopropyl-2-oxo-3-(3-(4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-1,2,4-triazol-3-yl)phenyl)pyrazolo[1,5-a]pyrimidin-5-yl)imidazolidin-1-yl)ethyl benzenesulfonate from step 1 (5 mL, 0.051 g, 0.071 mmol) was added pyrrolidine (2 mL) and the reaction stirred overnight at ambient temperature. The reaction was concentrated in vacuo and the material taken up in dichloromethane and washed with 1N NaOH. The combined organic layers were concentrated in vacuo and the residue chromatographed using 2% MeOH/dichloromethane to 5% MeOH/dichloromethane to yield (S)-4-isopropyl-1-(2-(pyrrolidin-1-yl)ethyl)-3-(3-(4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-1,2,4-triazol-3-yl)phenyl)pyrazolo[1,5-a]pyrimidin-5-yl)imidazolidin-2-one (0.041 g, 95%).

1. concentrationThe reaction was concentrated in vacuo
2. washwashed with 1N NaOH
3. concentrationThe combined organic layers were concentrated in vacuo
4. customthe residue chromatographed