反应详情

A mixture of 4-[2-(2,2,2-trifluoroethyl)guanidino]-2-(5-aminopentyl)pyrimidine (0.61 g.), chloroacetonitrile (0.17 g.) and triethylamine (0.23 g.) in EtOH (15 ml.) was heated under reflux for 7 hours. The solvent was evaporated and the residue was treated with sodium bicarbonate solution and extracted with EtOAc. The extract was dried (MgSO4) and evaporated to give an oil which was purified by medium pressure chromatography, eluting with 7.5% v/v MeOH in methylene chloride to give 4-[2-(2,2,2-trifluoroethyl)guanidino]-2-[5-cyanomethylaminopentyl]pyrimidine as a pale yellow solid which was used without further purification.

1. temperaturewas heated
2. temperatureunder reflux for 7 hours
3. customThe solvent was evaporated
4. additionthe residue was treated with sodium bicarbonate solution
5. extractionextracted with EtOAc
6. dry with materialThe extract was dried (MgSO4)
7. customevaporated
8. customto give an oil which
9. customwas purified by medium pressure chromatography
10. washeluting with 7.5% v/v MeOH in methylene chloride