反应详情

To a stirred solution of 4-aminomethyl-4-(4-iodo-phenyl)-piperidine-1-carboxylic acid tert-butyl ester (0.10 g, 0.24 mmol) in CH2Cl2 (0.5 mL) at room temperature under Ar was added a solution of 3,5-difluorophenylacetyl chloride (0.28 mL of a 1 M solution in CH2Cl2, 0.28 mmol) followed by pyridine (0.25 mL). The mixture was stirred at room temperature for 16 h then diluted with EtOAc (5 mL) and washed with saturated aqueous NaHCO3 (5 mL) and saturated brine (5 mL) and dried over Na2SO4. Filtration and rotary evaporation gave the crude 4-{[2-(3,5-difluoro-phenyl)-acetylamino]-methyl}-4-(4-iodo-phenyl)-piperidine-1-carboxylic acid tert-butyl ester (0.09 g, ˜65%).

1. washwashed with saturated aqueous NaHCO3 (5 mL) and saturated brine (5 mL)
2. dry with materialdried over Na2SO4
3. filtrationFiltration and rotary evaporation