A Versatile Catalyst-Free Perfluoroaryl Azide-Aldehyde-Amine Conjugation Reaction.
A Versatile Catalyst-Free Perfluoroaryl Azide-Aldehyde-Amine Conjugation Reaction.
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DOI：
10.1039/c8qm00516h
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发表时间：
2019-01
影响因子：
7
通讯作者：
Sheng Xie;Juan Zhou;Xuan Chen;Na Kong;Yanmiao Fan;Yang Zhang;G. Hammer;D. Castner;O. Ramström;Mingdi Yan
中科院分区：
文献类型：
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作者：
Sheng Xie;Juan Zhou;Xuan Chen;Na Kong;Yanmiao Fan;Yang Zhang;G. Hammer;D. Castner;O. Ramström;Mingdi Yan
涉及亲电活化的全氟芳基叠氮化物、可烯醇化的醛和胺的三组分反应在室温下在包括水性条件的溶剂中在没有任何催化剂的情况下容易地反应以产生稳定的脒缀合物。该反应的多功能性在没有预先保护羧基的氨基酸的缀合中以及在合成抗肿瘤纳米颗粒缀合物中得到证明。
A tri-component reaction, involving an electrophilically-activated perfluoroaryl azide, an enolizable aldehyde and an amine, reacts readily at room temperature without any catalysts in solvents including aqueous conditions to yield a stable amidine conjugate. The versatility of this reaction is demonstrated in the conjugation of an amino acid without prior protection of the carboxyl group, and in the synthesize antibiotic-nanoparticle conjugates.