Hagen M D, Scalfi-Happ C, Happ E, Chládek S
Department of Chemistry, Michigan Cancer Foundation, Detroit 48201.
Nucleic Acids Symp Ser. 1987(18):285-8.
A new synthetic approach to the title compounds is reported. It is based on the phosphotriester methodology and uses a unique combination of protecting groups (Fmoc and Ph for the aglycons; DMT, CPTr and Mthp for the carbohydrate hydroxy functions; 2-CIPh for the phosphodiester bonds; BPOC for amino acid). This enables selective deprotection of the blocked oligonucleotide intermediates in two steps (oximate and acid treatments) to yield the 2'(3')-O-aminoacyl oligoribonucleotides suitable for biochemical investigations.
报道了一种合成标题化合物的新方法。该方法基于磷酸三酯法,使用了保护基团的独特组合(苷元用Fmoc和Ph;碳水化合物羟基官能团用DMT、CPTr和Mthp;磷酸二酯键用2-CIPh;氨基酸用BPOC)。这使得可以通过两步(肟化和酸处理)对封闭的寡核苷酸中间体进行选择性脱保护,以得到适用于生化研究的2'(3')-O-氨酰基寡核糖核苷酸。