发明名称 PRODUCTION OF 5-TRIFLUOROMETHYL-2'-DEOXY-BETA-URIDINES
摘要 PURPOSE:To obtain the titled compound on an industrial scale at a low cost, by reacting a benzyl-deoxy-beta-uridine with N-trifluoromethyl-N- nitrosotrifluoromethane sulfonamide and subjecting the reaction product to deprotection reaction at the 5'-site, etc. CONSTITUTION:A 3'-O-benzyl-2'-deoxy-beta-uridine of formula II (R1 is trityl, substituted silyl, lower acyl or benzoyl; Bz is benzyl) is made to react with preferably 1-5 times mol of N-trifluoromethyl-N-nitrosotrifluoromethane sulfonamide usually under water-cooled condition or at room temperature for 30min-10 hr. The objective compound of formula I (R2 is H or benzyl) can be produced by subjecting the reaction product to deprotection at the 5'-site and, if necessary, to the elimination of 3'-benzyl group. The starting raw material of formula II is novel substance which can be produced e.g. according to the reaction formula.
申请公布号 JPS63145296(A) 申请公布日期 1988.06.17
申请号 JP19860294185 申请日期 1986.12.09
申请人 TAIHO YAKUHIN KOGYO KK 发明人 NOGUCHI KAZUHARU;YASUMOTO SANJI;KOBAYASHI KAZUHIRO
分类号 C07H19/073 主分类号 C07H19/073
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