反应详情

A mixture of N-(3′-hydroxy-biphenyl-4-yl)guanidine (550 mg), 2,4-dichloropyrimidine (146 mg) and potassium carbonate (196 mg) in DMF (8 ml) is stirred at rt for 20 h. This mixture is purified by preparative HPLC (gradient of water, 0.1% TFA/acetonitrile, 0.1% TFA from 80/20 to 0/100 on Nucleosil 100-10 C18 column). The fractions containing product are basified with 1 N NaOH to pH 8, evaporated and dried under reduced pressure. The residue is stirred in ethanol, the solvent is evaporated and dried under reduced pressure to afford crude N-[3′-(2-chloro-pyrimidin-4-yloxy)biphenyl-4-yl]-guanidine.

1. customThis mixture is purified by preparative HPLC (gradient of water, 0.1% TFA/acetonitrile, 0.1% TFA from 80/20 to 0/100 on Nucleosil 100-10 C18 column)
2. additionThe fractions containing product
3. customevaporated
4. customdried under reduced pressure
5. stirringThe residue is stirred in ethanol
6. customthe solvent is evaporated
7. customdried under reduced pressure