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Complex α-Pyrones Synthesized by a Gold-Catalyzed Coupling Reaction

机译:金催化偶联反应合成的复合α-吡喃酮

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摘要

We have been exploring a strategy for the synthesis of small molecules with properties that increase the probability of success in all facets of probe- and drug-discovery pipelines, including discovery, optimization, and manufacturing.[1] This strategy involves 1) the synthesis of building blocks with functionality suitable for subsequent coupling and pairing steps, 2) intermolecular coupling reactions that join the building blocks in all stereochemical combinations, and 3) intramolecular pairing reactions that join different combinations of functional groups to yield diverse skeletons.[2] Herein, we describe a multicomponent coupling reaction that we believe is well-suited for the coupling phase of this strategy, as it yields, among other substances, complex and diverse -pyrones, which are core elements found in many biologically active compounds.
机译:我们一直在探索一种合成小分子的策略,这种小分子的特性可以增加在探测和药物发现管线的所有方面(包括发现,优化和制造)的成功可能性。[1]该策略涉及1)合成具有适用于后续偶联和配对步骤功能的结构单元,2)以所有立体化学组合形式连接该结构单元的分子间偶联反应,和3)结合官能团的不同组合以产生不同的骨骼。[2]本文中,我们描述了一种多组分偶联反应,我们认为它非常适合该策略的偶联阶段,因为它除其他物质外还产生复杂多样的吡喃酮,这是许多生物活性化合物中的核心元素。

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