Ammonium Hydroxide → 8-Amino-3-bromoimidazo[1,2-a]pyrazine

Temperature

50 °C

To a solution of 3,5-dibromo-imidazo[1,2-a]pyrazine (D) (500 mg, 1.8 mmol) in THF (4 ml) was added NH4OH (4 ml). The mixture was heated at 50° C. in sealed tube overnight. Additional NH4OH (4 ml) was added to the reaction mixture and was heated at 50° C. in sealed tube overnight. The mixture was then cooled to rt, diluted with DCM (200 ml) and IN HCl (50 ml). The organic layer was washed with 10N NaOH, brine, dried and concentrated. The residue was purified on a silica gel column to afford 190 mg (yield 50%) of 3-bromo-imidazo[1,2-a]pyrazin-8-ylamine.

1. temperaturewas heated at 50° C. in sealed tube overnight
2. temperatureThe mixture was then cooled to rt
3. washThe organic layer was washed with 10N NaOH, brine
4. customdried
5. concentrationconcentrated
6. customThe residue was purified on a silica gel column

ORD record

ord-b181ee225a8f4457875217f656dc2c35

Source dataset

uspto-grants-2007_01

DOI

10.6084/m9.figshare.5104873.v1

Patent number

US07157460B2