A short and efficient synthesis of valsartan via a Negishi reaction

An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan(®)) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with prev...

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Detalles Bibliográficos
Autores principales: Ghosh, Samir, Kumar, A Sanjeev, Mehta, G N
Formato: Texto
Lenguaje:English
Publicado: Beilstein-Institut 2010
Materias:
Full Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2874312/
https://www.ncbi.nlm.nih.gov/pubmed/20502651
http://dx.doi.org/10.3762/bjoc.6.27
Descripción
Sumario:An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan(®)) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with previously reported syntheses.

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