Abstract

A simple method for the synthesis of functionalized tetrahydropyridines via TBPAc-catalyzed domino ring opening/cyclization of aziridines with isocyanides in the presence of malononitrile has been developed with high atom economy, in which 6-exo-dig cyclization process is observed. Tetrahydropyridines are quite remarkable owing to their multiple biological and pharmaceutical activities. This method provides rapid access to a diverse range of such compounds under mild conditions with good substrate tolerance and high efficiency.

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