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Identification of the first enantiopure Rac1–Tiam1 protein–protein interaction inhibitor and its optimized synthesis via phosphine free remote group directed hydroarylation

A phospine free hydroarylation reaction applied to norbornene derivatives is described for the first time and was exploited for the regioselective gram scale synthesis of AR-148, a known Rac1–Tiam1 PPI inhibitor. Umpolung conversion of the nitro group into free amine allowed the regiocontrol of the...

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Detalhes bibliográficos
Publicado no:Medchemcomm
Main Authors: Ruffoni, Alessandro, Ferri, Nicola, Pinto, Andrea, Pellegrino, Sara, Contini, Alessandro, Clerici, Francesca
Formato: Artigo
Idioma:Inglês
Publicado em: Royal Society of Chemistry 2018
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6396393/
https://ncbi.nlm.nih.gov/pubmed/30931091
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c8md00477c
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