Triphenylphosphine → 2-(4-{(1R,2S)-2-[2-(4-bromo-3-chlorophenoxy)ethyl]cyclopropyl}piperidin-1-yl)-5-(methoxymethyl)pyrimidine

Participants

Reaction Steps

2-[(1S,2R)-2-{1-[5-(methoxymethyl)pyrimidin-2-yl]piperidin-4-yl}cyclopropyl]ethanol (670 mg, 2.30 mmol) was dissolved in toluene (5 ml) and 4-bromo-3-chlorophenol (525 mg, 2.53 mmol), triphenylphosphine (905 mg, 3.45 mmol), and DIAD (671 μl, 3.45 mmol) added and the mixture stirred at RT overnight. The mixture was concentrated in vacuo and the residue purified by column chromatography on SiO2 using a Biotage 50M cartridge using a gradient eluant of 0-50% EtOAc:hexanes to afford the title compound. LC/MS (m/z): 481 (M+H)+.

Provenance & Evidence