| 摘要 |
NEW MATERIAL:The compound of formula I (X is halogen) and its salt. EXAMPLE:3'-Deoxy-3'-iodocytidine. USE:Carcinostatic agent. PREPARATION:The objective compound can be produced e.g. by (1) reacting the compound of formula II (R1 is lower acyl) (e.g. N-acetyl-cytosine) with a trimethylsilylation agent (e.g. hexamethyldisilazane) in a solvent such as dichloromethane under heating, (2) removing unreacted trimethylsilylation agent by e.g. distillation, (3) reacting the reaction product with the compound of formula III (R2 is lower acyl; R3 is 4-nitrobenzoyl, etc.) [e.g. 1,2-di-O-acetyl-3-deoxy-3- iodo-5-O-(p-nitrobenzoyl)-beta-D-ribofuranose] in the presence of a Lewis acid such as tin tetrachloride without separating the reaction product from the system and (4) deacylating the resultant compound of formula IV.
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