Desymmetrization of pibrentasvir for efficient prodrug synthesis

A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective N-Boc protection and formaldehyde adduct formation sequence, both enabled by cry...

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Bibliographic Details
Published in:Chem Sci
Main Authors: Voight, Eric A., Greszler, Stephen N., Hartung, John, Ji, Jianguo, Klix, Russell C., Randolph, John T., Shelat, Bhadra H., Waters, Jan E., DeGoey, David A.
Format: Artigo
Language:Inglês
Published: The Royal Society of Chemistry 2021
Subjects:
Chemistry
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC8317637/
https://ncbi.nlm.nih.gov/pubmed/34349971
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/d1sc02396a
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