Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step

1-Phenyl-1H-1,2,3-triazole 1 (ARUK3001185) was prepared on large scale from aniline 4 by application of both (1) a copper catalyzed azide–alkyne cycloaddition (CuAAC) with (trimethylsilyl)acetylene, and (2) a Clark modification of the Sakai reaction. The one-pot Sakai–Clark method with (MeO)(2)CHCH[...

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Detalles Bibliográficos
Autores principales: Atkinson, Benjamin N., Willis, Nicky J., Smith, Jennifer, Gill, Rebecca, Ali, Jody, Xu, Zhou, Lai, Ping-Shan, Fish, Paul V.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9478995/
https://www.ncbi.nlm.nih.gov/pubmed/36275171
http://dx.doi.org/10.1039/d2ra05132j

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