Abstract
The functionalization of a Csp2-H bond of an heteroarene with an alkyne represent one of the most attractive procedure for the late-stage functionalization of the aromatic core, due to the structural characteristics and synthetic versatility given by a triple carbon-carbon bond. The aim of this review is to cover the most significant results reported in the literature regarding the synthesis of alkynyl-substituted five-membered heteroarenes by selective direct Csp2-H alkynylation with 1-haloalkynes and analogues, or by cross-dehydrogenative alkynylation (CDA) with terminal alkynes, without making use of directing groups.
Keywords: CH activation, dehydrogenative coupling, inverse Sonogashira coupling, selectivity, heteroarenes, palladium catalyst, azoles.
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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