(Diethylamino)sulfur trifluoride → HCID 67060000, compound

Participants

Reaction Steps

(8-Hydroxy-8-phenyl-3-aza-bicyclo[3.2.1]oct-3-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]methanone (0.05 g, 0.12 mmol) in DCM (2 mL) was cooled to −78° C. under an atmosphere of nitrogen. Diethylaminosulphur trifluoride (0.05 mL) was added and the mixture stirred for 0.25 hour and allowed to warm to room temperature over 1 hour. The mixture was diluted with DCM and washed with water then dried over magnesium sulphate, filtered and the solvent removed by evaporation. The residue was purified by reverse phase HPLC and the fractions containing the desired products were combined and the solvent removed by lyophilisation to give the title compound as a white solid (0.02 g). LCMS m/z 382.1 [M+H]+. RT.=4.25 min (Analytical Method 2).

Provenance & Evidence