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Undirected, Selective Csp2-H Alkynylation of Five-membered Heteroarenes

Author(s):

Fabio Bellina*, Martina La Manna and Elisabetta Rosadoni  

Abstract:


The functionalization of Csp2-H bond of heteroarene with an alkyne represents one of the most attractive procedures 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 analogs, 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.

Affiliation:

Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Pisa, Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Pisa, Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Pisa



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