Lesiak K B, Uznanski B, Torrence P F
Section on Biomedical Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
Appl Biochem Biotechnol. 1997 Jul-Aug;67(1-2):33-44. doi: 10.1007/BF02787839.
To increase the accessibility of 8-bromo-2',5'-oligoadenylates, we developed a synthesis of 2'-5'-linked oligoriboadenylates containing varying numbers of 8-bromoadenosine residues based on the use of a CPG-LCA solid support and the phosphoramidite approach. Although N6-benzoyl protection was satisfactory for incorporation of nonmodified adenine residues into 2',5'-oligonucleotides, the effective incorporation of 8-bromoadenine into such 2',5'-linked oligomers required use of a non acyl protecting group. Amidine protection of the purine exocyclic amino function proved compatible with all aspects of the phophoramidite approach and with the hydroxyl protection groups employed.
为了提高8-溴-2',5'-寡腺苷酸的可及性，我们基于CPG-LCA固相载体和亚磷酰胺方法，开发了一种合成含有不同数量8-溴腺苷残基的2',5'-连接的寡聚核糖腺苷酸的方法。尽管N6-苯甲酰基保护对于将未修饰的腺嘌呤残基掺入2',5'-寡核苷酸是令人满意的，但将8-溴腺嘌呤有效掺入此类2',5'-连接的寡聚物中需要使用非酰基保护基团。嘌呤环外氨基功能的脒基保护被证明与亚磷酰胺方法的所有方面以及所采用的羟基保护基团兼容。
