【摘要】 以去氧氟尿苷、盐酸羟胺、氯甲酸正戊酯等为原料合成N4-戊氧碳酰-5’-脱氧-5-氟胞嘧啶,反应经加成、氢化、缩合、酰胺化等步骤得目标产物。产物经元素分析、IR、1H-NMR、13C-NMR、EI-MS确证。五步合成目标产物N4-戊氧碳酰-5’-脱氧-5-氟胞嘧啶总产率20.05%(以去氧氟尿苷计)。更多还原

【Abstract】 A novel synthesis of the new antitumour drug 5’-dexoxy-5-fluoro-N-(pentyloxy)cabonylcytidine is studied in this paper. Addition of hydroxylamine hydrochloride gave the compound (3),then putted hydrochloride and zinc in the constant temperature magnetic force stirrer via the reduction reaction gave 5’-deoxy-5-fluorocytidine (4),Condensation of (4) with acetone,which was subsequency converted to the corresponding pentyl chloride formate gained the derivative of the 5’-deoxy-5-fluorocytidine(6),then added the aqueous solution of hydrobromic acid and the target compound (1)has been gotten. A cost-efficient facile synthetic route is suitable for large-scale preparation of target compound,which has been provided through a five-step procedure starting from doxiflurdine in a total yield of 20.05%. And the structure verified by elementary analysis,IR,1H-NMR,13C-NMR and EI-MS.更多还原