反应详情

To a solution of 4-bromo-6,7-dihydro-5H-cyclopenta[c]pyridin-7-amine (650 mg, 3.05 mmol, 65% purity) and Et3N (400 mg, 3.97 mmol) in THF (20 mL) was added propionyl chloride (219 mg, 2.38 mmol) at 0° C. and stirring continued for 2 hours. Water (10 mL) and EtOAc (10 mL) were added and the aqueous layer was extracted with EtOAc (10 mL×3). The combined organic layers were dried over anhy. Na2SO4, filtered and concentrated in vacuo to give a crude product which was purified by column chromatography to afford the title compound (200 mg, 37.6%) as a white solid. MS: 270.9 (M+H+, 1Br).

1. extractionthe aqueous layer was extracted with EtOAc (10 mL×3)
2. customThe combined organic layers were dried over anhy
3. filtrationNa2SO4, filtered
4. concentrationconcentrated in vacuo
5. customto give a crude product which
6. customwas purified by column chromatography