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Expression, Purification, and Antimicrobial Activity of S100A12
Published on: May 13, 2017
Síntesis del antibiótico macrolido antifúngico (+) -roxaticin
David A Evans1, Brian T Connell
1Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA. Evans@Chemistry.Harvard.edu
Journal of the American Chemical Society
|September 4, 2003
Resumen
La síntesis total del macrolido antimicótico antifúngico roxaticina se logró mediante aldol y pasos de reducción. Los fragmentos clave fueron acoplados, seguidos de funcionalización y lactonización para completar la estructura de la roxaticina.
Área de la Ciencia:
- Química orgánica es la química orgánica.
- Química Medicinal La Química Medicinal es el campo de la Química Medicinal.
- Síntesis de Productos Naturales.
Sus antecedentes:
- La roxaticina es un antibiótico macrólido con propiedades antifúngicas.
- La estructura compleja de la roxaticina presenta un desafío sintético significativo.
Objetivo del estudio:
- Para lograr la síntesis total del antibiótico macrolido antifúngico roxaticin.
- Desarrollar una ruta sintética eficiente y convergente.
Principales métodos:
- Utilizó aldol y reacciones de reducción dirigidas para construir la columna vertebral de poliol.
- Empleado olefinación Julia y adición de metil cetona aldol para el acoplamiento de fragmentos.
- Se han incorporado porciones sensibles de polieno a través de reacciones de funcionalización.
Principales resultados:
- Con éxito sintetizó roxaticina a través de un enfoque convergente.
- Se obtienen buenos rendimientos en la etapa de lactonización.
- Completó la síntesis con la desprotección ácida.
Conclusiones:
- Se ha logrado con éxito la síntesis total de roxaticina.
- La estrategia sintética desarrollada es eficiente para la construcción de complejos antibióticos macrólidos.
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