反应详情

To (±)-2-(((5-fluoropyridin-2-yl)oxy)methyl)-7-azabicyclo[2.2.1]heptane (35 mg, 0.2 mmol) in DCM (2.5 mL) was added TEA (25 μL, 0.2 mmol)) followed by 2-(thiophen-2-yl)benzoyl chloride (40 mg, 0.2 mmol) in DCM (2.5 mL). After 18 h, the reaction was diluted with DCM and washed with H2O. The aqueous layer was extracted DCM (1×). The combined organics were dried (Na2SO4). Purification via silica gel chromatography (50-100% EtOAc in hexanes) gave the title compound (37 mg, 57%). MS (ESI) mass calcd. for C23H21FN2O2S, 408.1; m/z found 409.1 [M+H]+.

1. washwashed with H2O
2. extractionThe aqueous layer was extracted DCM (1×)
3. dry with materialThe combined organics were dried (Na2SO4)
4. customPurification via silica gel chromatography (50-100% EtOAc in hexanes)