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.
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