PRODUCTION OF 2'-DEOXY-5-TRIFLUOROMETHYL-BETA-URIDINE DERIVATIVE

PURPOSE:To obtain the subject derivative useful as an antitumor agent and an antiviral agent in high beta-selectivity and in a high yield by reacting specific compounds with each other in the presence of a copper compound as a catalyst and in the presence of fluoride ions in a specific solvent. CONS...

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Bibliographische Detailangaben
Hauptverfasser: KAWAUCHI KEIYA, FUKAZAWA NOBUYUKI, ISHIBASHI DAIKI
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:PURPOSE:To obtain the subject derivative useful as an antitumor agent and an antiviral agent in high beta-selectivity and in a high yield by reacting specific compounds with each other in the presence of a copper compound as a catalyst and in the presence of fluoride ions in a specific solvent. CONSTITUTION:5-Trifluoromethyl-2,4-bis(trimethylsilyloxy)pyrimidine of formula I is reacted with a 2-deoxy-alpha-D-erythro-pentofuranosyl chloride derivative of formula II (X is halogen; X , X are H, halogen) in the presence of fluoride ions and in the presence of a copper compound such as cupric chloride or cupric fluoride as a catalyst in chloroform solvent to afford the objective compound of formula III, namely 1-(2'-deoxy-beta-D-erythro-pentofuranosyl)-5- trifluoromethyluracil derivative.