反应详情

To a solution of bicyclo[2.2.1]heptane-2-carboxylic acid (102 mg, 0.73 mmol), 2-amino-indan-2-carboxylic acid ethyl ester (150 mg, 0.73 mmol), HATU (333 mg, 0.87 mmol) in anhydrous DMF (1 mL) is added DIPEA (1904, 1.10 mmol). The resulting solution is stirred at RT overnight. Water (10 mL) is poured into the reaction mixture and then extracted with EtOAc (3×5 mL). The combined organic layers are concentrated in vacuo. The residue is purified by flash column chromatography (12 g silica gel, gradient elution: 0-30% EtOAc in heptane) to give product (272) as yellow oil (148 mg, 62%).

1. extractionextracted with EtOAc (3×5 mL)
2. concentrationThe combined organic layers are concentrated in vacuo
3. customThe residue is purified by flash column chromatography (12 g silica gel, gradient elution: 0-30% EtOAc in heptane)