Two Facile General Methods for the Conjugation of Three Different Molecules,Bulletin of the Korean Chemical Society

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Two Facile General Methods for the Conjugation of Three Different Molecules
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2021-01-25 , DOI: 10.1002/bkcs.12208
Keumrok Oh ₁ , Dong Seok Shin ₂ , Hyeong Baik Kim ₁ , Uthaiwan Sirion ₃ , Dae Yoon Chi _{1,

2}

Affiliation

In the quest to synthesize compounds that are uniquely optimized for fighting each individual target disease, the importance of developing a new methodology for the bioconjugation of compounds with different functional groups or biological activities cannot be overemphasized. This study investigates two novel methods for click reaction: coupling a molecule with three functional compounds by repetitive copper(I) catalyzed azide/alkyne 1,3‐dipolar cycloadditions. Method A uses three copper(I) catalyzed azide/alkyne 1,3‐dipolar cycloadditions in series. Method B uses two copper(I) catalyzed azide/alkyne 1,3‐dipolar cycloadditions and one conjugation reaction of amine and isothiocyanate.

中文翻译：

三种不同分子结合的两种简便通用方法

为了合成针对每种目标疾病而独特优化的化合物，开发具有不同官能团或生物活性的化合物进行生物缀合的新方法的重要性不可过分强调。这项研究研究了两种新颖的点击反应方法：通过重复的铜（I）催化的叠氮化物/炔烃1,3-偶极环加成反应将分子与三种功能化合物偶联。方法A串联使用三个铜（I）催化的叠氮化物/炔烃1,3-偶极环加成反应。方法B使用两次铜（I）催化的叠氮化物/炔1,3-偶极环加成反应，以及一次胺和异硫氰酸酯的共轭反应。

更新日期：2021-02-24

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