反应详情

The 1[4-(methylsulfonyl)phenyl]-4,4′-bipiperidine (70 mg, 0.22 mmol) and cesium carbonate (212 mg, 0.65 mmol) were slurried in NMP (0.43 ml) and the Chlorobenzoxazole (20.3 mmol) added. The mixture was stirred at 120 C overnight. The slurry was diluted with 15% saturated sodium bicarbonate:water (40 ml) and extracted with DCM (3×25 ml). The combined organic fraction was washed with brine, dried over magnesium sulfate, filtered, and the volatiles removed in vac. The crude material was purified by chromatography on silica gel with 5% acetone:DCM to yield the titled compound. LRMS calc: 478.1 obs: 478.8, 480.8 (M+H).

1. extractionwater (40 ml) and extracted with DCM (3×25 ml)
2. washThe combined organic fraction was washed with brine
3. dry with materialdried over magnesium sulfate
4. filtrationfiltered
5. customthe volatiles removed in vac
6. customThe crude material was purified by chromatography on silica gel with 5% acetone