Ugi/Aldol Sequence: Expeditious Entry to Several Families of Densely Substituted Nitrogen Heterocycles


  • The authors thank the NIH (5RC2MH090878-02) for financial support, Dr. Gary S. Nichol and Dr. Sue A. Roberts (University of Arizona) for X-ray structural analyses and Kristen Keck for HPLC analyses.


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Complexity from simplicity: Nitrogen-containing heterocycles have been assembled by means of unprecedented domino processes designed to take advantage of diversity assembly using strategically decorated Ugi products (see scheme). The aldol reaction is the second common denominator which enables sequences of up to five steps in one pot, thus producing unique molecular architectures in rapid fashion.