反应详情

温度

40 °C

A mixture of 6-(2-Amino-5-bromo-phenylcarbamoyl)-5-aza-spiro[2.4]heptane-5-carboxylic acid benzyl ester and 6-(2-Amino-4-bromo-phenylcarbamoyl)-5-aza-spiro[2.4]heptane-5-carboxylic acid benzyl ester (1.446 g, 3.25 mmol) was dissolved in AcOH (20 mL) and the reaction mixture was stirred at 40° C. for 18 hours then concentrated under reduced pressure. The residue was dissolved in EtOAc and washed with saturated aqueous NaHCO3. The aqueous layer was extracted 2x with EtOAc and the combined organics were dried over MgSO4, filtered and concentrated to provide 6-(6-Bromo-1H-benzoimidazol-2-yl)-5-aza-spiro[2.4]heptane-5-carboxylic acid benzyl ester (1.385 g, 100%).

1. concentrationthen concentrated under reduced pressure
2. dissolutionThe residue was dissolved in EtOAc
3. washwashed with saturated aqueous NaHCO3
4. extractionThe aqueous layer was extracted 2x with EtOAc
5. dry with materialthe combined organics were dried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated