(6-Bromo-5-fluoropyridin-2-yl)-tert-butylamine → 6-Bromo-5-fluoropyridin-2-amine

A solution of (6-bromo-5-fluoropyridin-2-yl)-tert-butylamine (46 mg, 0.19 mmol) in DCE (2 mL) and TFA (2 mL) was heated at 120° C. for 10 min in a microwave reactor, and then concentrated under reduced pressure. The residue was taken up in MeOH and loaded onto an Isolute® SCX-2 cartridge (5 g). The cartridge was washed with MeOH then the desired product eluted with 2 M NH3 in MeOH to give 6-Bromo-5-fluoropyridin-2-ylamine as an off-white solid (25 mg, 71%). 1H NMR (400 MHz, CHCl3-d): δ 7.21 (dd, J=8.7, 7.2 Hz, 1 H); 6.39 (dd, J=8.7, 2.7 Hz, 1 H); 4.89-3.75 (s, 2 H).

1. concentrationconcentrated under reduced pressure
2. washThe cartridge was washed with MeOH
3. washthe desired product eluted with 2 M NH3 in MeOH

ORD record

ord-aa9865eff359439080384e92029a619a

Source dataset

uspto-grants-2012_05

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US08173650B2