Ligand-Mediated Highly Effective and Selective C−N Coupling for Synthesizing Bioactive N-Aryltriazole Acyclonucleosides

详细信息    查看全文

• 作者：Yuting Fan ; Yi Xia ; Jingjie Tang ; Palma Rocchi ; Fanqi Qu ; Juan Iovanna ; Ling Peng
• 刊名：Organic Letters
• 出版年：2010
• 出版时间：December 17, 2010
• 年：2010
• 卷：12
• 期：24
• 页码：5712-5715
• 全文大小：214K
• 年卷期：v.12,no.24(December 17, 2010)
• ISSN：1523-7052

文摘

N-aryltriazole nucleosides are new chemical entities with potential biological activity. The two phosphor ligands, Synphos and Xantphos, had a selective and effective impact on Pd-catalyzed C−N coupling with the 5- and 3-bromotriazole acyclonucleoside isomers, affording the corresponding and otherwise difficult to achieve N-aryltriazole nucleosides with good to excellent yields. In addition, two of the synthesized nucleosides showed superior anticancer activity against drug-resistant pancreatic cancer, compared to the reference drug gemcitabine.