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Issue 2, 2013
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Applications of asymmetric organocatalysis in medicinal chemistry

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In the last decade, organocatalysis, the use of small chiral organic molecules as catalysts, has proven to be a valuable and attractive tool for the synthesis of enantiomerically enriched molecules. A number of organocatalysts and processes, such as one-pot, tandem, cascade or multicomponent reactions, have been reported to date. Furthermore, the many advantages of organocatalysis – robust, non-toxic, affordable, inert atmosphere, easy reaction manipulation, etc. – allow the preparation of bioactive compounds using simple and metal-free procedures, thus avoiding false positives in the biological evaluation. This mini-review focuses on medicinal chemistry programs that have synthesized biologically active compounds using one or more organocatalytic steps. In this respect, the potential of organocatalytic methods for enabling the chemical synthesis of important medicinal targets will be highlighted.

Graphical abstract: Applications of asymmetric organocatalysis in medicinal chemistry

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The article was received on 11 Sep 2012 and first published on 15 Nov 2012

Article type: Review Article
DOI: 10.1039/C2CS35380F
Chem. Soc. Rev., 2013,42, 774-793

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    Applications of asymmetric organocatalysis in medicinal chemistry

    J. Alemán and S. Cabrera, Chem. Soc. Rev., 2013, 42, 774
    DOI: 10.1039/C2CS35380F

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