Rozners E Z, Rekis A Kh, Kumpin'sh V Kh, Bizdena E O
Bioorg Khim. 1990 Nov;16(11):1531-6.
The N-acyl, 5'-O-trityl (MeOTr, (MeO)2Tr, Me3Tr), 2'-O-benzoyl (and anisole) nucleosides were prepared by selective aroylation of N,5'-protected nucleosides. By means of the reverse-phase microcolumn liquid chromatography it was shown that the rate of the aryl 2'----3'-isomerisation is lower in case of 2'-anisoylnucleosides and depends on structure of the 5'-O-protecting group. The prepared synthons were used for the manual H-phosphonate solid-phase synthesis of oligoribonucleotides (6-10-mers).
通过对N,5'-保护的核苷进行选择性芳酰化反应制备了N-酰基、5'-O-三苯甲基(甲氧基三苯甲基、二甲氧基三苯甲基、三甲氧基三苯甲基)、2'-O-苯甲酰基(及苯甲醚)核苷。通过反相微柱液相色谱法表明,2'-苯甲醚核苷的芳基2'→3'-异构化速率较低,且取决于5'-O-保护基的结构。所制备的合成子用于手动H-膦酸酯固相合成寡核糖核苷酸(6至10聚体)。