6-(Trifluoromethyl)benzo[b]thiophene-2-carbonyl chloride → 2,2,2-Trifluoro-1-(4-(1-(6-(trifluoromethyl)benzo[b]thiophene-2-carbonyl)azetidin-3-yl)piperazin-1-yl)ethanone

Participants

Reaction Steps

A solution of 6-(trifluoromethyl)benzo[b]thiophene-2-carbonyl chloride (2.03 mmol, 537 mg) in CH2Cl2 (5 mL) was added to a solution of 1-(4-azetidin-3-yl-piperazin-1-yl)-2,2,2-trifluoro-ethanone (2.26 mmol, 700 mg) and TEA in CH2Cl2 (15 mL) at 0° C. The resulting mixture was allowed to warm to room temperature and was stirred for 2 h. Following workup and extraction, the residue was purified by flash column chromatography (silica gel, 3% methanol/CH2Cl2) to yield 2,2,2-trifluoro-1-(4-(1-(6-(trifluoromethyl)benzo[b]thiophene-2-carbonyl)azetidin-3-yl)piperazin-1-yl)ethanone.

Provenance & Evidence