1-Ethynyl-3-fluorobenzene → Adx 10059

Participants

Reaction Steps

To a solution of Cul (41 mg, 0.2 mmol) in triethylamine (12 ml) were added 2-bromo-4,6-dimethyl-pyridin-3-ylamine (870 mg, 4.33 mmol), (PPh3)2PdCl2 (152 mg, 0.22 mmol), and 1-ethynyl-3-fluorobenzene (500 μl, 4.33 mmol). The reaction mixture was stirred for 30 min. at room temperature and for 3 h under reflux. The solvent was evaporated and the crude residue was purified by flash chromatography (cyclohexane/ethyl acetate 4:1) to yield 745 mg (3.10 mmol, 72%) of (2-(3-fluoro-phenylethynyl)-4,6-dimethyl-pyridin-3-yl)amine as a brown solid.

Provenance & Evidence