反应详情

温度

100 °C

2-Amino-N-(4-tert-butyl-benzyl)-5-chloro-N-[2-(3-trifluoromethyl-phenyl)-ethyl]-benzamide (80 mg, 0.164 mmol), bromo-acetonitrile (21 mg, 0.172 mmol) and sodium hydrogen catbonat (17 mg, 01.96 mmol) were suspended in ethanol (21 ml) and heated to 100° C. for 3 days. The reaction mixture was cooled to RT, filtered and the precipitate was washed with ethanol. The solvent of the filtrate was concentrated in vacuo to give a residue which was purified by flash column chromatography (heptane/ethyl acetate 7:3) to yield the desired product (26 mg, 30%) as a yellow solid. MS (ISP) 526.2 (M−H)−.

1. temperatureThe reaction mixture was cooled to RT
2. filtrationfiltered
3. washthe precipitate was washed with ethanol
4. concentrationThe solvent of the filtrate was concentrated in vacuo
5. customto give a residue which
6. customwas purified by flash column chromatography (heptane/ethyl acetate 7:3)