Giovanninetti G, Garuti L, Cavrini V, Amorosa M
Farmaco Sci. 1976 Dec;31(12):871-9.
3,6-Anhydro-1-deoxy-1-(5-bromouracil-1-yl)-D-mannitol (II) and 3,6-anhydro-1-deoxy-1-(5-iodouracil-1-yl)-D-mannitol (III) were prepared by direct halogenation of the corresponding bis-homonucleosides; the 5-fluoro isomer (V) was prepared by N-alkylation of 5-fluorouracil by 2-o-acetyl-3,6-anhydro-4,5-o-isopropylidene-1-o-p-tolysulfonyl-D-mannitol in dimethylsulfoxide in the presence of potassium carbonate followed by hydrolysis of the protective groups in an acid medium. The ultraviolet spectroscopy, mass spectrometry and nuclear magnetic resonance studies of these compounds are described and the results of pharmacological tests on L 1210 leukemic cells are given.
3,6-脱水-1-脱氧-1-(5-溴尿嘧啶-1-基)-D-甘露糖醇（II）和3,6-脱水-1-脱氧-1-(5-碘尿嘧啶-1-基)-D-甘露糖醇（III）通过相应的双同核苷直接卤化制备；5-氟异构体（V）通过在碳酸钾存在下，于二甲基亚砜中，用2-O-乙酰基-3,6-脱水-4,5-O-异亚丙基-1-O-对甲苯磺酰基-D-甘露糖醇对5-氟尿嘧啶进行N-烷基化反应制备，随后在酸性介质中水解保护基团。描述了这些化合物的紫外光谱、质谱和核磁共振研究，并给出了对L 1210白血病细胞的药理测试结果。
