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基于功能化氧杂双环[2.2.1]庚烯的化学文库的合成。

Synthesis of a functionalized oxabicyclo[2.2.1]-heptene-based chemical library.

作者信息

Luesse Sarah B, Wells Gregg, Miller Jeanne, Bolstad Erin, Bergmeier Stephen C, McMills Mark C, Priestley Nigel D, Wright Dennis L

机构信息

Department of Chemistry & Biochemistry, Ohio University, Athens, Ohio 45701, USA.

出版信息

Comb Chem High Throughput Screen. 2012 Jan;15(1):81-9. doi: 10.2174/138620712798280835.

Abstract

The 7-oxabicyclo[2.2.1]heptene ring system is a common structural motif in many pharmacologically interesting molecules. We recognized the potential to employ this highly oxygenated and conformationally-restricted scaffold in diversity-oriented synthesis to generate a library of non-chiral but topologically complex compounds. Herein, we report the synthesis and biological evaluation of two 96-member tricyclic libraries containing the oxabicyclo[2.2.1]heptene framework using acetal formation as the key step.

摘要

7-氧杂双环[2.2.1]庚烯环系是许多具有药理学意义的分子中常见的结构基序。我们认识到在多样化合成中利用这种高度氧化且构象受限的骨架来生成非手性但拓扑结构复杂的化合物库的潜力。在此,我们报道了以缩醛形成作为关键步骤,合成并生物学评价了两个包含氧杂双环[2.2.1]庚烯骨架的96元三环化合物库。

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