Design and Synthesis of Fsp3-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening

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• 作者：Silvia Stotani ; Christoph Lorenz ; Matthias Winkler ; Federico Medda ; Edwige Picazo ; Raquel Ortega Martinez ; Anna Karawajczyk ; Jorge Sanchez-Quesada ; Fabrizio Giordanetto
• 刊名：ACS Combinatorial Science
• 出版年：2016
• 出版时间：June 13, 2016
• 年：2016
• 卷：18
• 期：6
• 页码：330-336
• 全文大小：445K
• 年卷期：0
• ISSN：2156-8944

文摘

The exploration of innovative chemical space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biologically relevant metabolites and show attractive features, such as molecular compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available commercial reagents and robust chemical transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented.