An intramolecular inverse electron demand Diels–Alder approach to annulated α-carbolines

Intramolecular inverse electron demand cycloadditions of isatin-derived 1,2,4-triazines with acetylenic dienophiles tethered by amidations or transesterifications proceed in excellent yields to produce lactam- or lactone-fused α-carbolines. Beginning with various isatins and alkynyl dienophiles, a p...

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Detalles Bibliográficos
Autores principales: Ma, Zhiyuan, Ni, Feng, Woo, Grace H C, Lo, Sie-Mun, Roveto, Philip M, Schaus, Scott E, Snyder, John K
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Beilstein-Institut 2012
Materias:
Full Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3388871/
https://www.ncbi.nlm.nih.gov/pubmed/23015831
http://dx.doi.org/10.3762/bjoc.8.93
Descripción
Sumario:Intramolecular inverse electron demand cycloadditions of isatin-derived 1,2,4-triazines with acetylenic dienophiles tethered by amidations or transesterifications proceed in excellent yields to produce lactam- or lactone-fused α-carbolines. Beginning with various isatins and alkynyl dienophiles, a pilot-scale library of eighty-eight α-carbolines was prepared by using this robust methodology for biological evaluation.

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