Divergent Synthesis and Real-Time Biological Annotation of Optically Active Tetrahydrocyclopenta[c]pyranone Derivatives

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• 作者：Shawn D. Nelson Jr. ; Mathias J. Wawer ; Stuart L. Schreiber
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：December 16, 2016
• 年：2016
• 卷：18
• 期：24
• 页码：6280-6283
• 全文大小：349K
• ISSN：1523-7052

文摘

Sp³-rich compounds are underrepresented in libraries for probe- and drug-discovery, despite their promise of extending the range of accessible molecular shapes beyond planar geometries. With this in mind, a collection of single-enantiomer bicyclic, fused cyclopentenones underpinned by a complexity-generating Pauson–Khand cyclization was synthesized. A fingerprint of biological actions of these compounds was determined immediately after synthesis using real-time annotation−a process relying on multiplexed measurements of alterations in cell morphological features.