| 摘要 |
1,209,654. Pyrimidone nucleosides. MERCK & CO. Inc. 2 July, 1968 [3 July, 1967], No. 31574/68. Heading C2C. The novel α- and #-anomers of nucleosides of the formula -wherein L is a C 1-5 alkoxy, hydroxy, amino. C 1-5 alkyl substituted amino, M is as defined for L or H, C 1-5 alkyl, halogen or halogenated C 1-5 alkyl and either Y is H and Z is C 1-5 alkyl or Z is H and Y is C 1-5 alkyl, may be prepared by reacting a compound of the formula wherein each of R<SP>1</SP>, R<SP>11</SP>, and R<SP>111</SP> is acyl and X is halogen, with a compound of the formula wherein V is H or C 1-5 alkyl, to form an intermediate of the formula wherein W is C 1-5 alkoxy or OH and subjecting this intermediate to (a) treatment with a solvent in the presence of a base, when W = OH, or (b) reaction with ammonia, C 1-5 alkylamine or di-(C 1-5 alkyl) amine when W=alkoxy. The novel nucleosides demonstrate antiviral activity, are capable of inhibiting RNA synthesis, have favourable cytotoxicity characteristics and show resistance to the action of adenosine deaminase. |
