Transition-metal-catalyzed intramolecular cyclization of amido(hetero)arylboronic acid aldehydes to isoquinolinones and derivatives
We report an innovative and simple three step high yielding synthesis of a library of 14 chiral isoquinolinone and azepinone derivatives with benzyl, pyridyl and thiophene cores starting from amidoarylboronic acid aldehydes. These products have potential for treating neuro-degenerative diseases. The...
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| Outros Autores: | , |
| Formato: | article |
| Idioma: | eng |
| Publicado em: |
2016
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| Assuntos: | |
| Texto completo: | http://hdl.handle.net/10174/16611 |
| País: | Portugal |
| Oai: | oai:dspace.uevora.pt:10174/16611 |
| Resumo: | We report an innovative and simple three step high yielding synthesis of a library of 14 chiral isoquinolinone and azepinone derivatives with benzyl, pyridyl and thiophene cores starting from amidoarylboronic acid aldehydes. These products have potential for treating neuro-degenerative diseases. The key reaction in this synthetic pathway was an efficient metal-catalyzed (with Rh, Cu and Pd catalysts) intramolecular cyclization. A maximum yield of 87% was obtained using a Rh(I) catalyst. |
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