(Diethylamino)sulfur trifluoride → HCID 90204253, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-[4-(2,2,2-Trifluoro-ethoxy)-pyridin-3-yl]-cyclobutanol (example 108b, 1.7 g, 6.88 mmol) in dry dichloromethane (25.0 ml) under an argon atmosphere cooled down to 0° C. was added DAST (1.36 ml, 10.3 mmol). The reaction mixture was stirred at 0° C. for 30 minutes. The reaction was quenched by addition of a 2M aqueous solution of sodium carbonate and the bi-phasic mixture was stirred for 20 minutes. The bi-phasic mixture was transferred into a separatory funnel and the organic phase was collected. The organic phase was dried over sodium sulfate and evaporated down to dryness to yield the title compound (1.68 g, 98%); MS (ESI, m/z): 250.4 (M+H+). The crude material was used without any purification for the next step.

Provenance & Evidence