反应详情

A solution of [4-(2-tert-butylphenyl)piperazin-1-yl](oxo)acetic acid (Example 44, 0.300 g, 1.03 mmol), 2-amino-2-methylpropan-1-ol (0.111 g, 1.24 mmol), EDCI (0.238 g, 1.24 mmol) and HOBt (0.168 g, 1.24 mmol) in acetonitrile (5 mL) was stirred at room temperature for 16 h. The reaction mixture was poured into saturated sodium hydrogen carbonate solution and extracted with ethyl acetate. The organic layer was washed with saturated sodium hydrogen carbonate solution and brine, dried over MgSO4, and the solvent was evaporated under reduced pressure to give the crude product. The product was purified by flash column chromatography (silica gel, n-hexane/ethyl acetate=80:20 to 40:60) to provide 2-[4-(2-tert-butylphenyl)piperazin-1-yl]-N-(2-hydroxy-1,1-dimethylethyl)-2-oxoacetamide (0.302 g, 81%) as a white amorphous.

1. extractionextracted with ethyl acetate
2. washThe organic layer was washed with saturated sodium hydrogen carbonate solution and brine
3. dry with materialdried over MgSO4
4. customthe solvent was evaporated under reduced pressure
5. customto give the crude product
6. customThe product was purified by flash column chromatography (silica gel, n-hexane/ethyl acetate=80:20 to 40:60)