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.
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