(Diethylamino)sulfur trifluoride → HCID 89717376, compound

Participants

Reaction Conditions

Reaction Steps

A suspension of 2-{4-[5-(1-ethyl-1H-pyrazol-4-ylamino)-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-phenyl}-propan-2-ol (138 mg, 0.38 mmol) in dichloromethane (3 ml) is cooled to −78° C. Diethylaminosulfurtrifluoride (201 μl, 1.52 mmol) is added. The reaction mixture is allowed to reach room temperature over 1 hour. The reaction mixture is evaporated and the residue is treated with water and saturated sodium hydrogen carbonate solution. The solids are filtered off and chromatographed on a silica gel column with dichloromethane/methanol as eluent to afford (1-ethyl-1H-pyrazol-4-yl)-{3-[4-(1-fluoro-1-methyl-ethyl)-phenyl]-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl}-amine (“A128”) as yellow powder; HPLC/MS1.93 min (A), [M+H] 367;

Provenance & Evidence