反应详情

2-{(1S,2R)-2-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]cyclopropyl}ethanol (75 mg, 0.266 mmol) was dissolved in toluene (1 ml) and 1-(azetidin-1-yl)-2-(4-hydroxy-2-methoxyphenyl)ethanone (59 mg, 0.069 mmol), triphenylphosphine (105 mg, 0.399 mmol), and DIAD (78 μl, 0.399 mmol) added and the mixture stirred at RT overnight. The mixture was concentrated in vacuo and the residue purified by column chromatography using a Biotage RP C18 cartridge (30 g) using a gradient eluant of 0-100% water:acetonitrile+0.1% TFA to afford the title compound. LC/MS (m/z): 485 (M+H)+. GPR119 Human EC50: 7.1 nM.

1. concentrationThe mixture was concentrated in vacuo
2. customthe residue purified by column chromatography