Reaction of isatin with alkylating agents with acidic methylenes

The reaction of isatin (1) with different alkyl halides 2 and alkaline carbonates in aprotic polar solventsleads mainly to N-alkyl derivatives 3. The use of alkylating agents that have acidic methylenes leads tocompetitive formation of the corresponding epoxide 5. The formation of 5 is favored by lo...

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Detalles Bibliográficos
Autores: Shmidt, María Sol, Perillo, Isabel Amalia, González, Mercedes, Blanco, María de Las Mercedes
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2012
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/198422
Acceso en línea:http://hdl.handle.net/11336/198422
Access Level:acceso abierto
Palabra clave:4-QUINOLINONES
EPOXYOXINDOLES
ISATIN
N- AND O-ALKYL DERIVATIVES
REARRANGEMENT
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
Descripción
Sumario:The reaction of isatin (1) with different alkyl halides 2 and alkaline carbonates in aprotic polar solventsleads mainly to N-alkyl derivatives 3. The use of alkylating agents that have acidic methylenes leads tocompetitive formation of the corresponding epoxide 5. The formation of 5 is favored by low-polarity solvents at low temperatures and strong bases. Epoxides 5c, d obtained using NaEtOH/EtOH at 0?5 C are transformed into the corresponding 4-quinolinones 6 at higher temperatures. The use of Ag2CO3 allows obtaining compounds 3 as major products, along with varying amounts of labile O-alkyl derivatives 4 and dimerization products.