FC1C=C(C=CC=1F)CN1C(=[O:16])C2C(=CC=C(I)C=2)N(C)C1=O.C(N(C(C)C)CC)(C)C.[F:33][C:34]1[CH:39]=[CH:38][C:37]([CH2:40][C:41]#[CH:42])=[CH:36][CH:35]=1.O>CN(C=O)C.[Cu]I>[F:33][C:34]1[CH:39]=[CH:38][C:37]([CH:40]([OH:16])[C:41]#[CH:42])=[CH:36][CH:35]=1
To 0.5 g (1.06 mmol) 3-(3,4-Difluoro-benzyl)-6-iodo-1-methyl-1H-quinazoline-2,4-dione and 0.52 g (4.2 mmol) di-isopropyl ethylamine in 15 ml DMF is added bis-triphenylphosphine palladium di-chloride (catalytic) followed by CuI (catalytic). 0.15 g (1.3 mmol) 1-fluoro-4-prop-2-ynyl-benzene is added and the mixture is heated to 70° C. for 6 hours. The mixture is allowed to cool to room temperature and stir overnight. Water is added and the mixture stirred 30 minutes. Filtered and triturated solid in hot EtOAc and filtered. Purified by flash chromatography (EtOAc/hexane eluent).
Wird geladen…
