1,2-Dichloroethane → 1-(Azetidin-1-yl)-2-(3-fluoro-4-hydroxyphenyl)ethanone

Participants

Reaction Steps

To a solution of (3-fluoro-4-methoxyphenyl)acetic acid (0.94 g, 5.52 mmol) in 8 ml anhydrous DMF at RT was added azetidine (0.379 g, 6.63 mmol) and N,N-diisopropylethylamine (2.89 ml, 16.6 mmol), and EDC (1.59 g, 8.29 mmol) was added into the solution and stirred at RT for 4 hrs. The residue was purified by reverse-phase HPLC (SunFire Prep C18 OBD 5 um 19×100 mm column; 10-100% acetonitrile in 0.1% formic acid in water gradient), to give the title compound. LC/MS (m/z) 210.2 (M+15)+.

Provenance & Evidence