Direct Anodic <i>N</i> ‐α Hydroxylation: Accessing Versatile Intermediates for Azanucleoside Derivatives
Direct Anodic <i>N</i> ‐α Hydroxylation: Accessing Versatile Intermediates for Azanucleoside Derivatives
复制标题
直接阳极 <i>N</i> -α 羟基化：获取氮杂核苷衍生物的多功能中间体
DOI：
10.1002/ajoc.202100756
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发表时间：
2022
影响因子：
2.7
通讯作者：
Chiba Kazuhiro
中科院分区：
文献类型：
--
作者：
Kurose Yuma;Okamoto Kazuhiro;Okada Yohei;Kitano Yoshikazu;Chiba Kazuhiro
呋喃糖环氧取代的人工核苷即使不掺入寡核苷酸中也显示出独特的药理活性，并被用作抗癌和抗病毒药物。这种核苷的实际合成路线对加强（寡核苷酸）治疗学的发展具有特殊的重要性。在此，我们证明了在水介质中直接阳极n‐α羟基化是可能的，以实现这些多功能中间体对氮杂核苷衍生物的合成。
Furanose ring oxygen‐substituted artificial nucleosides show unique pharmacological activities even without incorporation into oligonucleotides, and are used as anticancer and antiviral agents. Practical synthetic routes to such nucleosides are of exceptional importance to enhance the development of (oligo)nucleotide therapeutics. Herein, we demonstrate that direct anodicN‐α hydroxylation is possible in aqueous media to realize the practical synthesis of these versatile intermediates for azanucleoside derivatives.