反应详情

To the solution of methyl octahydrocyclopenta[c]pyrrole-3a-carboxylate (1.0 g, 5.91 mmol) in EtOH (10.0 mL) was added DIPEA (2.80 mL, 16.12 mmol) at rt and the mixture stirred at rt for 10 min followed by addition of 5-bromo-2-chloropyrimidine (1.10 g, 5.37 mmol). The reaction was heated up to 70° C. for 2 h. After completion (by TLC), solvent was evaporated and the crude residue purified over 100-200 M silica-gel using 7.0% EtOAc:hexane to obtain the desired product as a white solid (0.80 g, 45%). MS: 326.19 [M+H]+.

1. temperatureThe reaction was heated up to 70° C. for 2 h
2. customAfter completion (by TLC), solvent was evaporated
3. customthe crude residue purified over 100-200 M silica-gel