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Pyrrolo[2,1-f][1,2,4]triazin-4-amine: Synthesis, C7-Functionalization, and NH2-Derivatization via Buchwald-Hartwig-Type Coupling

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Autor(es):
Duraes Pereira, Vinicius Rodrigues ; Vargas, Geovana Fontes ; Braga, Taniris Cafiero ; dos Santos, Juliana Alves ; Clososki, Giuliano Cesar ; Nallar, Jaime Alberto Rabi ; Pinho, Vagner Dantas ; Amarante, Giovanni Wilson
Número total de Autores: 8
Tipo de documento: Artigo Científico
Fonte: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY; v. N/A, p. 6-pg., 2025-10-24.
Resumo

An optimized gram-scale synthetic route to pyrrolo[2,1-f][1,2,4]triazin-4-amine is reported, affording an overall yield of 85%. Furthermore, regioselective C7-functionalization is achieved via both organometallic and direct strategies, whereas NH2-derivatization proceeds through Buchwald-Hartwig-type coupling, providing derivatives in isolated yields ranging from 8% to >99%. These advancements enhance synthetic accessibility and facilitate efficient structural diversification of this significant N-heterocycle. (AU)

Processo FAPESP: 22/05327-7 - Explorando o espaço químico medicinal de aromáticos com ferramentas sintéticas altamente seletivas
Beneficiário:Giuliano Cesar Clososki
Modalidade de apoio: Auxílio à Pesquisa - Regular