Potassium Fluoride → 4-[6-ethynyl-2-(2-fluoroethoxy)-1H-1,3-benzodiazol-1-yl]pyrimidin-2-amine

Participants

Reaction Steps

A solution of 4-[2-(2-fluoroethoxy)-6-[2-(trimethylsilyl)ethynyl]-1H-1,3-benzodiazol-1-yl]pyrimidin-2-amine (100 mg, 0.27 mmol) and potassium fluoride (64 mg, 0.68 mmol) in methanol (3 mL) was stirred at 50° C. for 3 hr. The reaction mixture was concentrated under vacuum and the residue was diluted with 30 mL of ethyl acetate. The resulting mixture was washed with 3×10 mL of water and the organic layer was dried over anhydrous sodium sulfate and concentrated under vacuum to give 70 mg (87%) of 4-[6-ethynyl-2-(2-fluoroethoxy)-1H-1,3-benzodiazol-1-yl]pyrimidin-2-amine as a yellow solid: LC-MS: m/z=+298 (M+H)+.

Provenance & Evidence