反应详情

温度

50 °C

(R)-cyclohexyl(phenyl)[1-(piperidin-4-ylmethyl)-1H-1,2,4-triazol-3-yl]methanol (Preparation 4, 2.00 g, 5.64 mmol) and di-tert-butyl (9-bromononyl)imidodicarbonate (U.S. Pat. No. 4,167,167, 2.38 g, 5.64 mmol) were dissolved in acetonitrile (60 ml) and triethylamine (2.35 ml, 16.9 mmol) added. After stirring at 50° C. for 18 hours, the solvent was removed in vacuo, and the residue purified by column chromatography on silica gel eluting with dichloromethane:methanol:880 ammonia (98:2:0.2, by volume) to furnish the title compound as a clear oil, in 60% yield, 2.6 g (contains 10% of other triazole regio-isomer)

1. customthe solvent was removed in vacuo
2. customthe residue purified by column chromatography on silica gel eluting with dichloromethane