Wu Minwan, El-Kattan Yahya, Lin Tsu-Hsing, Ghosh Ajit, Kumar V Satish, Kotian Pravin L, Cheng Xiaogang, Bantia Shanta, Babu Yarlagadda S, Chand Pooran
BioCryst Pharmaceuticals, Inc., Birmingham, Alabama 35244, USA.
Nucleosides Nucleotides Nucleic Acids. 2005;24(10-12):1569-85. doi: 10.1080/15257770500265315.
Various C-1'-substituted acyclic N9 adenine nucleosides were prepared from 9-[(1-hydroxymethyl)(3-monomethoxytrityloxy)propyl]-N6-monomethoxytrityladenine. The hydroxymethyl was modified to the phosphonomethoxy derivative, and the 3-monomethoxytrityloxy was converted to hydroxyl, methoxy, azido, and amino. Other substituents, such as ethyl and ea-hydroxyethyl were also prepared. The resulting phosphonomethoxy derivatives were converted to prodrugs.
从9-[(1-羟甲基)(3-单甲氧基三苯甲基氧基)丙基]-N6-单甲氧基三苯甲基腺嘌呤制备了各种C-1'-取代的无环N9腺嘌呤核苷。羟甲基被修饰为膦酰基甲氧基衍生物,3-单甲氧基三苯甲基氧基被转化为羟基、甲氧基、叠氮基和氨基。还制备了其他取代基,如乙基和α-羟乙基。所得的膦酰基甲氧基衍生物被转化为前药。