Palladium-mediated C-N, C-C, and C-O functionalization of azolopyrimidines: a new total synthesis of variolin B

A new total synthesis of the alkaloid variolin B is achieved by a selective and sequential palladium-mediated functionalization of a trihalo-substituted pyrido[30 ,20 :4,5]pyrrolo[1,2-c]pyrimidine. This intermediate is obtained by a new heterocyclization reaction between an appropriate bromomethyl a...

Descripción completa

Detalles Bibliográficos
Autores: Baeza García, Alejandro, Mendiola Serena, Javier, Burgos García, Carolina, Álvarez-Builla Gómez, Julio, Vaquero López, Juan José|||0000-0002-3820-9673
Tipo de recurso: artículo
Fecha de publicación:2008
País:España
Institución:Universidad de Alcalá (UAH)
Repositorio:e_Buah Biblioteca Digital Universidad de Alcalá
Idioma:inglés
OAI Identifier:oai:ebuah.uah.es:10017/2653
Acceso en línea:http://hdl.handle.net/10017/2653
https://dx.doi.org/10.1016/j.tetlet.2008.04.063
Access Level:acceso abierto
Palabra clave:Variolin B
Total synthesis
Palladium-mediated C-N, C-C and C-O
pyrido[3 ',2 ': 4,5]pyrrolo[1,2-c]pyrimidine
N-tosylmethyl dichloro-formimide
Sponge kirkpatrickia-varialosa
Deoxyvariolin-B
Bond formation
Alkaloids
Core
Derivatives
Ethers
Chemistry, Organic
Bioquímica
Ciencia
Biochemistry
Science
Descripción
Sumario:A new total synthesis of the alkaloid variolin B is achieved by a selective and sequential palladium-mediated functionalization of a trihalo-substituted pyrido[30 ,20 :4,5]pyrrolo[1,2-c]pyrimidine. This intermediate is obtained by a new heterocyclization reaction between an appropriate bromomethyl azaindole and N-tosylmethyl dichloroformimide. The methodology may be effective for the synthesis of some analogs by substitution on the relatively unexplored C4 and C9 positions of the alkaloid.