van Boom J H, Burgers P M, van der Marel G, Verdegaal C H, Wille G
Nucleic Acids Res. 1977 Apr;4(4):1047-63. doi: 10.1093/nar/4.4.1047.
A combination of two different methods for the synthesis of oligoribonucleotides, i.e. the two-step phosphotriester method with 2-chlorophenyl phosphate as bifunctional phosphate source and the modified triester method with 2,2,2-trichloroethyl 2-chlorophenyl phosphorochloridate as monofunctional phosphate source, is applied for the synthesis of the fully-protected hexaribonucleotide A-C-C-U-C-C. The two-step method is used for the synthesis of the required dinucleotide monophosphates 9, 10 and 11. Application of the modified triester method for the coupling of the oligonucleotide blocks results in the formation of the fully-protected hexamer 15. Furthermore, attention is paid to 2,4,6-triisopropylbenzenesulphonyl 4-nitroimidazolide as a new condensing agent for the coupling of larger oligonucleotide blocks.
两种不同的合成寡核糖核苷酸的方法相结合,即使用磷酸二(2-氯苯基)酯作为双功能磷酸源的两步磷酸三酯法和使用2,2,2-三氯乙基 2-氯苯基磷酰氯作为单功能磷酸源的改良三酯法,用于合成完全保护的六核糖核苷酸A-C-C-U-C-C。两步法用于合成所需的二核苷酸单磷酸酯9、10和11。使用改良三酯法进行寡核苷酸片段的偶联,得到完全保护的六聚体15。此外,还关注了2,4,6-三异丙基苯磺酰基 4-硝基咪唑作为一种用于较大寡核苷酸片段偶联的新型缩合剂。