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通过三组分缩合作为关键反应高效合成新型双三唑糖缀合物。

An efficient synthesis of novel bis-triazole glycoconjugates via a three-component condensation as a key reaction.

作者信息

Cheng Jie, Gu Zhenlong, He Caiyu, Jin Jie, Wang Lijun, Li Guojun, Sun Bei, Wang Hui, Bai Jun

机构信息

Office of Scientific Research, Anhui Provincial Institute for Food and Drug Control, Hefei 230022, China.

School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China.

出版信息

Carbohydr Res. 2015 Sep 23;414:72-7. doi: 10.1016/j.carres.2015.07.004. Epub 2015 Jul 23.

Abstract

Novel bis-triazole glycoconjugates were designed and prepared successfully via 5 steps from propargyl per-O-acetyl-β-d-glucoside or xyloside (total yield of 48-53%), after utilizing a three-component condensation of propargyl per-O-acetyl-β-d-glycoside, formaldehyde, and sodium azide as a key step to synthesize 2-hydroxymethyl-2H-1,2,3-triazole glycoconjugates. The developed bis-triazole glycoconjugates would be crucial in antivirus pharmacology and chemical biology.

摘要

新型双三唑糖缀合物通过五步反应从炔丙基全-O-乙酰基-β-D-葡萄糖苷或木糖苷成功设计并制备出来(总产率为48-53%),其中利用炔丙基全-O-乙酰基-β-D-糖苷、甲醛和叠氮化钠的三组分缩合反应作为关键步骤来合成2-羟甲基-2H-1,2,3-三唑糖缀合物。所开发的双三唑糖缀合物在抗病毒药理学和化学生物学中将至关重要。

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