反应详情

温度

115 °C

A mixture of (S)-[1-(3-hydroxy-phenyl)-ethyl]-carbamic acid tert-butyl ester (1 g, 4.2 mmol), 2-chloro-pyrazine (0.58 g, 5.1 mmol), potassium carbonate (powder, 1.4 g, 10.1 mmol), copper iodide (325 mesh powder, 0.6 g, 3.2 mmol) and pyridine (5 mL) was heated at 115° C. for 24 h. CH2Cl2 (100 mL) was added, and the reaction mixture was diluted with CH2Cl2 (100 mL), filtered through celite, and rinse with CH2Cl2 (2×50 mL). The filtrate was concentrated in vacuo and the residue was purified by flash column chromatography on silica gel eluting with 1:1/Hexane:EtOAc to give the title product (1.5 g, quantitative yield).

1. filtrationfiltered through celite
2. washrinse with CH2Cl2 (2×50 mL)
3. concentrationThe filtrate was concentrated in vacuo
4. customthe residue was purified by flash column chromatography on silica gel eluting with 1:1/Hexane