合成路线:Hydrogenation of 4-amino-1-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl-1,3,5-triazin-2(1H)-one (I) in ethanolic hydrogen chloride and palladium on charcoal catalyst produces 4-amino-5,6-dihydro-1-(beta-D-arabinofuranosyl)-1,3,5-triazin-2(1H)-one hydrochloride (II).This is treated with bis (trimethylsilyl)trifluoroacetamide in acetonitrile solution to give the pentakis-trimethylsilyl derivative (III).Conversion to arabinosyl-5-azacytosine as the tetrakis-trimethylsilyl derivative (IV) is complete following 53 h of reflux of the silylation solution.The solution is then evaporated.The residual is boiled with methanol to remove the trimethylsilyl groups.
参考文献标题:FAZARABINE < Rec INN; USAN >
文献作者:King,S.A.; Grem,J.L.
参考来源:Drugs Fut 1989,14(1),20
合成路线:Hydrogenation of 4-amino-1-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl-1,3,5-triazin-2(1H)-one (I) in ethanolic hydrogen chloride and palladium on charcoal catalyst produces 4-amino-5,6-dihydro-1-(beta-D-arabinofuranosyl)-1,3,5-triazin-2(1H)-one hydrochloride (II).This is treated with bis (trimethylsilyl)trifluoroacetamide in acetonitrile solution to give the pentakis-trimethylsilyl derivative (III).Conversion to arabinosyl-5-azacytosine as the tetrakis-trimethylsilyl derivative (IV) is complete following 53 h of reflux of the silylation solution.The solution is then evaporated.The residual is boiled with methanol to remove the trimethylsilyl groups.
参考文献标题:The synthesis and antitumor activity of arabinosyl-5-azacytosine
文献作者:Beisler,J.A.; Abbasi,M.M.; Driscoll,J.S.
参考来源:Biochem Pharmacol 1977,262469-72
产品链接: CAS No. 65886-71-7››