Tetrahydrofuran → 3-Ethynylpyridin-2-amine

Participants

Reaction Steps

To a THF (120 mL) solution of 3-trimethylsilanylethynyl-pyridin-2-ylamine (5.9 g) described in Manufacturing Example 1-1 was added tetrabutylammonium fluoride (34 mL: 1M THF solution) at 0° C., which was stirred for 25 minutes at room temperature. Water was added at 0° C. to the reaction solution, which was then extracted with ethyl acetate. The organic layer was washed with water and saturated brine, then dried over anhydrous magnesium sulfate, and filtered, after which the filtrate was concentrated under a reduced pressure. The residue was purified by silica gel chromatography (heptane:ethyl acetate=1:1) to obtain the titled compound (2.3 g).

Provenance & Evidence