Cyclopropylamine → 5-Bromo-N-cyclopropylpyridin-2-amine

Temperature

80 °C

To a sealed tube was added 5-bromo-2-fluoropyridine (1.25 g, 7.10 mmol) and cyclopropylamine (5.0 mL, 72 mmol). Upon heating at 80° C. for 48 hours the reaction was complete. The contents of the tube were transferred to a round bottom flask and concentrated in vacuo. The remaining residue was dissolved in dichloromethane and washed twice with saturated sodium bicarbonate and twice with brine. The organics were dried over sodium sulfate, filtered and concentrated in vacuo to afford the title compound (1.13 g, 75%) as a tan solid.

1. customThe contents of the tube were transferred to a round bottom flask
2. concentrationconcentrated in vacuo
3. dissolutionThe remaining residue was dissolved in dichloromethane
4. washwashed twice with saturated sodium bicarbonate and twice with brine
5. dry with materialThe organics were dried over sodium sulfate
6. filtrationfiltered
7. concentrationconcentrated in vacuo

ORD record

ord-2d2e22ead0cd40ed813cf1029e9ffbeb

Source dataset

uspto-grants-2016_01

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US09227971B2