反应详情

To a solution of (S)-1-(2-hydroxyethyl)-4-isopropyl-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 (Example 25, Step 6; 0.160 g, 0.284 mmol) in pyridine was added 4-methylbenzene-1-sulfonyl chloride (0.136 g, 0.711 mmol) and the reaction stirred overnight at ambient temperature. The reaction was next concentrated in vacuo and the reaction chromatographed using EtOAc as eluent to yield (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 4-methylbenzenesulfonate (0.14 g, 68.7%).

1. concentrationThe reaction was next concentrated in vacuo
2. customthe reaction chromatographed