Abstract
Biginelli reaction is the most classical and frequently employed method for facile and diverse synthesis of 3,4- dihydropyrimidinones and thiones (DHPMs)-a class of privileged heterocyclic scaffolds possessing meritorious biological and pharmacological functions. Owing to the presence of a chiral centre in DHPMs and the discovered distinction in biological activity of DHPMs isomers, accessing chiral DHPMs of optical purity constitutes a core issue of particular importance in the research of Biginelli reaction. Following the rapid progress of modern organic synthesis, catalytic asymmetric Biginelli reaction has gradually evolved as the mainstream method instead of early kinetic resolution for acquiring enantiomerically enriched. In the present paper, the advances in catalytic asymmetric Biginelli reaction, including advances in metal catalysis as well as organocatalysis, are comprehensively reviewed.
Keywords: Asymmetric, Biginelli reaction, catalytic, DHPMs, enantioselective.
Graphical Abstract
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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