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

Silvia Stotani, Christoph Lorenz, Matthias Winkler, Federico Medda, Edwige Picazo, Raquel Ortega Martinez,Anna Karawajczyk, Jorge Sanchez-Quesada, and Fabrizio Giordanetto

ACS Comb. Sci., DOI: 10.1021/acscombsci.6b00005

Abstract:
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.

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