Synthesis of 3,4-Dihydroquinazolinones via Base-Promoted Formal [4 + 2] Cycloadditions

3,4-dihydroquinazolin-2(1H)-one (3,4-DHQ) is a key structural motif found in many biologically active molecules. Although several synthetic methods have been developed to date, harsh reaction conditions, and/or metal toxic reagents are often required. In this work, a general, metal-free methodology...

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Detalles Bibliográficos
Autores: Torres Oya, Sergio|||0000-0002-1003-519X, Fernández Rodríguez, Manuel Ángel|||0000-0002-0120-5599, Zurro de la Fuente, Mercedes|||0000-0003-1222-7926
Tipo de recurso: artículo
Fecha de publicación:2025
País:España
Institución:Universidad de Alcalá (UAH)
Repositorio:e_Buah Biblioteca Digital Universidad de Alcalá
Idioma:inglés
OAI Identifier:oai:ebuah.uah.es:10017/66138
Acceso en línea:http://hdl.handle.net/10017/66138
https://dx.doi.org/10.1002/adsc.70056
Access Level:acceso abierto
Palabra clave:3,4-dihydroquinazolinones
[4 þ 2] cycloadditions
Aza-ortho-quinone methides
Isocyanates
Química
Chemistry
Descripción
Sumario:3,4-dihydroquinazolin-2(1H)-one (3,4-DHQ) is a key structural motif found in many biologically active molecules. Although several synthetic methods have been developed to date, harsh reaction conditions, and/or metal toxic reagents are often required. In this work, a general, metal-free methodology for the synthesis of 3,4-DHQs is described. This novel protocol relies on a formal [4 + 2] cycloaddition of in situ formed aza-ortho-quinone methides and isocyanates leading to a wide variety of 3,4-DHQs in yields up to 98%.