1,2-Dichloroethane → (5-Bromo-6-methyl-2-(methylamino)pyridin-3-yl)(3-hydroxyazetidin-1-yl)methanone

Participants

Reaction Steps

To 5-bromo-6-methyl-2-(methylamino)nicotinic acid (0.2 g, 0.816 mmol) in DMF (3 mL) were added azetidin-3-ol (0.119 g, 1.632 mmol), HOBt (0.154 g, 1.143 mmol), and EDC (0.235 g, 1.224 mmol), followed by N-ethyl-N-isopropylpropan-2-amine (0.426 mL, 2.448 mmol). The reaction mixture was stirred for 18 hours at room temperature. The crude reaction mixture was subsequently diluted with EtOAc, washed with brine, dried over Na2SO4, and concentrated by rotary evaporation to give the title compound, which was used without further purification (0.15 g).

Provenance & Evidence