一锅法合成N_4-乙酰-5-氟胞苷的新工艺研究

Study on new synthetic technology of N_4-acetyl-5-fluorocytidine in one-pot

介绍了合成N4-乙酰氟胞苷的新工艺。在溶剂中5-氟胞嘧啶∶六甲基二硅胺烷(HMDS)∶三甲基氯硅烷(TMCS)∶四乙酰核糖(摩尔比)=1∶0.8∶0.8∶1,以无水四氯化锡为催化剂,一锅法合成5-氟胞苷,并以甲醇为溶剂直接用乙酐酰化得到N4-乙酰氟胞苷。总收率77%以上。

A new process of N4-acetyl-5-fluorocytidine producing in one-pot was introduced.Taking 5-fluorocytosine（5-Fc）,hexamethyl disilylamine（HMDS）,trimethyl chlorosilane（TMCS） and 1,2,3,5-tetraacetyl-beta-D-ribofuranose（TAR）（molar ratio=1∶ 0.8∶ 0.8∶ 1） into solvent such as acetonitrile,using anhydrous stannic chloride as catalyst to produce 5-fluorocytidine.Then,5-fluorocytidine was acylated in methanol using acetic anhydride to gain N4-acetyl-5-fluorocytidine directly.Total yield was up to 77%.