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The Cyclic Nitronate Route to Pharmaceutical Molecules: Synthesis of GSK’s Potent PDE4 Inhibitor as a Case Study

An efficient asymmetric synthesis of GlaxoSmithKline’s potent PDE4 inhibitor was accomplished in eight steps from a catechol-derived nitroalkene. The key intermediate (3-acyloxymethyl-substituted 1,2-oxazine) was prepared in a straightforward manner by tandem acylation/(3,3)-sigmatropic rearrangemen...

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Detalles Bibliográficos
Autores principales: Pospelov, Evgeny V., Golovanov, Ivan S., Ioffe, Sema L., Sukhorukov, Alexey Yu.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7464803/
https://www.ncbi.nlm.nih.gov/pubmed/32784502
http://dx.doi.org/10.3390/molecules25163613

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