Triethylamine → 2-Bromo-1-(4-(piperidin-1-yl)phenyl)ethanone

Temperature

0 °C

2,2-Dibromo-1-[4-(1-piperidinyl)phenyl]ethanone (3 g, 8.3 mmol) (from Step A above) was dissolved in tetrahydrofuran (15 mL), and cooled to 0° C. To the resulting solution were added dropwise diethylphosphite (1.13 mL, 8.7 mmol) and triethylamine (1.21 mL, 8.7 mmol) in tetrahydrofuran (7 mL) at 0° C. with stirring. The mixture was slowly warmed to room temperature and stirred for 6 h. The reaction mixture was concentrated in vacuo and poured into ice/water. The precipitate was collected by filtration, washed with water and dried in vacuo to provide 2-bromo-1-[4-(1-piperidinyl)phenyl]ethanone (2.3 g, 100% yield).

1. temperatureThe mixture was slowly warmed to room temperature
2. stirringstirred for 6 h
3. concentrationThe reaction mixture was concentrated in vacuo
4. additionpoured into ice/water
5. filtrationThe precipitate was collected by filtration
6. washwashed with water
7. customdried in vacuo

ORD record

ord-ff4256aaf0c04c6c9ceb8c97dc41cecd

Source dataset

uspto-grants-2006_08

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US07094896B2