反应详情

A solution of 2-(3-pyrazin-2-yl-4,5-dihydro-1H-pyrazol-5-yl)phenol (0.10 g, 4.2 mmol), 5-(2-([(tert-butoxycarbonyl)amino]methyl)phenyl)thiophene-2-carboxylic acid (0.134 g, 4.02 mmol), and EDCI (0.116 g, 6.06 mmol) in DCM (4 mL) was allowed to stir at rt for 6 h. The reaction was quenched by the addition of water and the organic and aqueous solutions were separated. The aqueous solution was extracted with EtOAc. The organic solutions were combined, dried over Na2SO4, filtered and concentrated. The residue was purified by column chromatography to give tert-butyl [2-(5-{[5-(2-hydroxyphenyl)-3-pyrazin-2-yl-4,5-dihydro-1H-pyrazol-1-yl]carbonyl}-2-thienyl)benzyl]carbamate (0.50 g, 23%). LCMS: (FA) ES+ 556.2.

1. customThe reaction was quenched by the addition of water
2. customthe organic and aqueous solutions were separated
3. extractionThe aqueous solution was extracted with EtOAc
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated
7. customThe residue was purified by column chromatography