反应详情

温度

120 °C

Cesium carbonate (489 mg, 1.5 mmol) was added to a solution of 3-hydroxy-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide (159 mg, 0.5 mmol) and 5-(azetidin-1-ylcarbonyl)-2-chloro-1,3-thiazole (152 mg, 0.75 mmol) in acetonitrile (5 mL) and the stirred mixture heated at 120° C. in a microwave reactor for 1 hour. The mixture was cooled to RT and ambient pressure, the acetonitrile evaporated in vacuo, the residue partitioned between water (25 mL) and ethyl acetate (50 mL), the organic layer washed with brine, dried (MgSO4) and evaporated to a residue which was chromatographed on silica, eluting with ethyl acetate, to give the desired product (181 mg).

1. temperatureThe mixture was cooled to RT
2. customambient pressure, the acetonitrile evaporated in vacuo
3. customthe residue partitioned between water (25 mL) and ethyl acetate (50 mL)
4. washthe organic layer washed with brine
5. dry with materialdried (MgSO4)
6. customevaporated to a residue which
7. customwas chromatographed on silica
8. washeluting with ethyl acetate