Water → HCID 59853676, compound

Participants

Reaction Steps

To a suspension of Trimethylsulfoxonium iodide (21.9 mg, 0.1 mmol) in dry DMSO (300 uL) was added Potassium tert-butoxyde (11.3 mg, 0.101 mmol) portionwise. A solution of (2-Isopropenyl-5-methanesulfonyl-phenyl)-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-methanone; Example 44 (20 mg, 0.0442 mmol) in dry THF (200 uL) was prepared separately and then added to the above suspension dropwise at room temperature. The reaction mixture was stirred at room temperature for 1 hour and then at 60° C. for 20 hours.The it was cooled down to rt and a solution of Trimethylsulfoxonium iodide (21.9 mg, 0.1 mmol) and Potassium tert-butoxyde (11.3 mg, 0.101 mmol) in dry DMSO (300 uL) was slowly added. Water was added and the solution was extracted 2 times with Ethylacetate. The combined organic phases were washed with water (3 times), dried over Na2SO4 ,filtered and the solvent was removed in vacuo. The residue was chromatographed on SiO2 Eluent: Heptane/EtOAc to provide the title compound (4.2 mg, 20%, white solid; Solid; M+H=467.2)

Provenance & Evidence