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Issue 39, 2014
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Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification

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Abstract

A strategy for generating diverse collections of small molecules has been developed that features a multicomponent assembly process (MCAP) to efficiently construct a variety of intermediates possessing an aryl aminomethyl subunit. These key compounds are then transformed via selective ring-forming reactions into heterocyclic scaffolds, each of which possesses suitable functional handles for further derivatizations and palladium-catalyzed cross coupling reactions. The modular nature of this approach enables the facile construction of libraries of polycyclic compounds bearing a broad range of substituents and substitution patterns for biological evaluation. Screening of several compound libraries thus produced has revealed a large subset of compounds that exhibit a broad spectrum of medicinally-relevant activities.

Graphical abstract: Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification

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Publication details

The article was received on 22 Apr 2014, accepted on 23 Jul 2014 and first published on 19 Aug 2014


Article type: Review Article
DOI: 10.1039/C4OB00835A
Citation: Org. Biomol. Chem., 2014,12, 7659-7672
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    Evolution of a strategy for preparing bioactive small molecules by sequential multicomponent assembly processes, cyclizations, and diversification

    J. J. Sahn, B. A. Granger and S. F. Martin, Org. Biomol. Chem., 2014, 12, 7659
    DOI: 10.1039/C4OB00835A

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