申请人:Kings College London
公开号:US05436331A1
公开(公告)日:1995-07-25
A process for protecting the 2'-hydroxyl of a nucleoside, which can then be used in the chemical synthesis of polyribonucleotides, comprising the reacting of a protected nucleoside of formula I ##STR1## wherein B is a nucleoside heterocyclic base and R' is a hydroxyl-protecting group, with 1-N-aryl-4-alkoxy-1,2,5,6-tetrahydropiperidine of formula II ##STR2## wherein Ar is an aryl group possessing an electron-withdrawing substituent which renders said protecting group acid labile and R is C.sub.1 -C.sub.4 alkyl, in the presence of an acid catalyst and a solvent to yield the compound of formula II below: ##STR3##
一种保护核苷2'-羟基的过程,然后可用于聚核糖核苷酸的化学合成,包括将具有以下式I的受保护核苷(其中B为核苷杂环碱基,R'为羟基保护基团)与具有以下式II的1-N-芳基-4-烷氧基-1,2,5,6-四氢哌啶(其中Ar为具有使所述保护基具有酸性易裂性的电子提取取代基的芳基,R为C.sub.1-C.sub.4烷基),在酸催化剂和溶剂存在下反应,得到以下式II的化合物: