Phosphorus tribromide → 4-Bromo-2-(trifluoromethyl)pyrimidine
Reaction equation
[F:1][C:2]([F:11])([F:10])[C:3]1[N:8]=[C:7](O)[CH:6]=[CH:5][N:4]=1.P(Br)(Br)[Br:13]>>[Br:13][C:7]1[CH:6]=[CH:5][N:4]=[C:3]([C:2]([F:11])([F:10])[F:1])[N:8]=1Participants
3
Conditions
- Temperature
- 150 °C
Procedure
The 2-(trifluoromethyl)pyrimidin-4-ol (328 mg, 2.0 mmol) and PBr3 (0.188 mL, 2.0 mmol) were mixed and heated at 150° C. for 3 h. The reaction was cooled down and quenched with ice water, extracted with DCM (20 mL×2) to yield the titled compound. The organic phase was concentrated and crude material was purified by preparative TLC with 20% Acetone:Hexane to yield titled compound.
Workup
- temperatureThe reaction was cooled down
- customquenched with ice water
- extractionextracted with DCM (20 mL×2)
Sources & evidence
- ORD record
- ord-e259c119de3f45838672877634131a0f
- Source dataset
- uspto-grants-2013_03
- Patent number
- US08399485B2
Reaction notes
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