4-(4-BROMOPHENYL)PYRIMIDIN-2-AMINE

Add 4-bromo-2-aminopyrimidine (8.70 g, 50.0 mmol), 4-bromo-phenylboronic acid (11.0 g, 55.0 mmol), tetratriphenylphosphine palladium (2.89 g, 2.5 mmol), cesium carbonate (10.8 g , 33.0 mmol) was dissolved in methanol / water (200 mL, 1/1), refluxed and stirred for 12 h.Ethyl acetate and water were added.After the organic phase was separated, it was washed twice with saturated saline.The solvent was removed by vacuum rotary evaporation, and the residue was purified by silica gel chromatography to obtain solid compound 8a (7.50 g, 30.0 mmol) in a 60% yield.Compound 8a (12.5 g, 50.0 mmol), 2-bromo-2-phenylacetophenone (16.5 g, 60.0 mmol), NaHCO3(5.04g, 60.0mmol) were dissolved in isopropanol (100 mL), refluxed and Stir for 12h.The isopropanol was removed by rotary evaporation in vacuo, and then dichloromethane (60 mL) and water (30 mL) were added to the solid residue.After the organic phase was separated, it was washed twice with saturated saline.The solvent was removed by vacuum rotary evaporation, and the residue was purified by silica gel chromatography to obtain solid compound 8b (13.2 g, 31.0 mmol) in a yield of 62%.To a slurry of

Molecular Weight:250.09
XLogP3:2.2
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:1
Exact Mass:248.99016
Monoisotopic Mass:248.99016
Topological Polar Surface Area:51.8
Heavy Atom Count:14
Complexity:180
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes