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Issue 9, 2009
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High-throughput synthesis of azide libraries suitable for direct “click” chemistry and in situ screening

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Abstract

A key challenge in current drug discovery is the development of high-throughput (HT) amenable chemical reactions that allow rapid synthesis of diverse chemical libraries of enzyme inhibitors. The Cu(I)-catalyzed, 1,3-dipolar cycloaddition between an azide and an alkyne, better known as “click chemistry”, is one such method that has received the most attention in recent years. Despite its popularity, there is still a lack of robust and efficient chemical strategies that give access to diverse libraries of azide-containing building blocks (key components in click chemistry). We report herein a highly robust and efficient strategy for high-throughput synthesis of a 325-member azide library. The method is highlighted by its simplicity and product purity. The utility of the library is demonstrated with the subsequent “click” synthesis of the corresponding bidentate inhibitors against PTP1B.

Graphical abstract: High-throughput synthesis of azide libraries suitable for direct “click” chemistry and in situ screening

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Publication details

The article was received on 04 Feb 2009, accepted on 10 Feb 2009 and first published on 11 Mar 2009


Article type: Paper
DOI: 10.1039/B902338K
Citation: Org. Biomol. Chem., 2009,7, 1821-1828
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    High-throughput synthesis of azide libraries suitable for direct “click” chemistry and in situ screening

    R. Srinivasan, L. P. Tan, H. Wu, P. Yang, K. A. Kalesh and S. Q. Yao, Org. Biomol. Chem., 2009, 7, 1821
    DOI: 10.1039/B902338K

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