反应详情

To a solution of 515 mg (1.98 mmol) 4-(5-amino-3-tert-butyl-pyrazol-1-yl)-benzoic acid and 259 μL (2.98 mMol) morpholine in 8 mL THF, 495 mg (2.58 mmol) of EDC are added at rt. The reaction is stirred at rt for 2 h. After completion, the resulting reaction mixture is concentrated and the residue is taken up in CH2Cl2, washed with brine (2×), dried and concentrated. The residual crude product is purified by flash chromatography (SiO2, CH2Cl2/MeOH; gradient 0-5% MeOH) to give the title compound as an off white powder. MS: [M+1]+=329.

1. customAfter completion, the resulting reaction mixture
2. concentrationis concentrated
3. washwashed with brine (2×)
4. customdried
5. concentrationconcentrated
6. customThe residual crude product is purified by flash chromatography (SiO2, CH2Cl2/MeOH; gradient 0-5% MeOH)