Synthesis of novel isoxazoline and isoxazolidine derivatives: carboxylic acids and delta bicyclic lactones via the nucleophilic addition of bis(trimethylsilyl)ketene acetals to isoxazoles

Bis(trimethylsilyl)ketene acetals readily react with activated N-triflyl isoxazoles to selectively afford novel isoxazoline or isoxazolidine derivatives. The regioselectivity of the reaction strongly depends on the substrate substituents. When the isoxazole is substituted at the 5-position by a meth...

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Detalles Bibliográficos
Autores: Cecilio Alvarez, Ricardo Ballinas-Indili, Morelia Eunice Lopez Reyes, Rubén A. Toscano
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2021
País:México
Institución:Universidad Nacional Autónoma de México
Repositorio:Repositorio del Instituto de Química, UNAM
Idioma:inglés
OAI Identifier:oai:rdu.iquimica.unam.mx:20.500.12214/1301
Acceso en línea:http://rdu.iquimica.unam.mx/handle/20.500.12214/1301
Access Level:acceso abierto
Palabra clave:info:eu-repo/classification/cti/2
Ketene acetals
Isoxazoline
Isoxazolidine
Lactone
N-triflyl activation
Descripción
Sumario:Bis(trimethylsilyl)ketene acetals readily react with activated N-triflyl isoxazoles to selectively afford novel isoxazoline or isoxazolidine derivatives. The regioselectivity of the reaction strongly depends on the substrate substituents. When the isoxazole is substituted at the 5-position by a methyl or phenyl group, the lactonization product, i.e., the isoxazolidine derivative, is formed as a result of double nucleophilic addition of the ketene acetal. When the isoxazole is not substituted, the main product is the corresponding carboxylic acid, i.e., the isoxazoline derivative.