反应详情

To a solution of 3-methyl-thiophene-2,5-dicarboxylic acid 2-methyl ester (0.1 g, 0.5 mmol) and 3-hydroxyphenethylamine hydrochloride (105 mg, 0.6 mmol) in DMF (5 ml) was added at rt triethylamine (0.21 ml, 1.5 mmol), HOBT (81 mg, 0.6 mmol) and HBTU (230 mg, 0.6 mmol). The mixture was stirred at rt for 1 h, then quenched with 1NHCl and extracted with EtOAc. The layers were separated. The organic layer was washed with brine, then dried over Na2SO4 and concentrated under reduced pressure. The residue was purified by flash chromatography with 15-65% EtOAc in hexane to afford the desired product (260 mg, 81% yield).

1. customquenched with 1NHCl and
2. extractionextracted with EtOAc
3. customThe layers were separated
4. washThe organic layer was washed with brine
5. dry with materialdried over Na2SO4
6. concentrationconcentrated under reduced pressure
7. customThe residue was purified by flash chromatography with 15-65% EtOAc in hexane