公开(公告)号：US20060199959A1

公开(公告)日：2006-09-07

申请号：US10567696

申请日：2004-07-29

申请人： Giorgio Bertolini ,  Patrizia Castoldi ,  Mauricio Deleo ,  Marco Frigerio ,  Maurizio Velati

发明人： Giorgio Bertolini ,  Patrizia Castoldi ,  Mauricio Deleo ,  Marco Frigerio ,  Maurizio Velati

IPC分类号： C07F9/6512

CPC分类号： C07H19/06 ,  C07H19/16 ,  Y02P20/55

摘要： A process for preparing 2′,3′-didehydro-2′,3′-dideoxynucleosides and 2′,3′-dideoxynucleosides is described, which comprises the reductive elimination reaction of a compound of formula in which X, Y, P′ is H or a protecting group and B is a natural or modified, optionally substituted purine or pyrimidine base or a five- or six-membered monocyclic or eleven- or twelve-membered bicyclic, optionally substituted heterocyclic system containing at least one nitrogen atom, by reaction with zinc metal and a suitable activating agent, characterized in that the divalent zinc is removed by precipitation, from an organic phase, of the corresponding zinc sulfide, by adding a solution of a mineral sulfide to the organic phase.

摘要翻译： 描述了制备2'，3'-二脱氢-2'，3'-双脱氧核苷和2'，3'-二脱氧核苷的方法，其包括式X化合物的还原消除反应，其中X，Y，P' H或保护基，B是通过反应的天然或修饰的任选取代的嘌呤或嘧啶碱基或五元或六元单环或十一元或十二元双环，任选取代的含有至少一个氮原子的杂环体系 其中锌金属和合适的活化剂，其特征在于，通过向有机相中加入无机硫化物溶液，通过从有机相中沉淀出相应的硫化锌来除去二价锌。