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
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author Ghosh, Samir
Kumar, A Sanjeev
Mehta, G N
author_facet Ghosh, Samir
Kumar, A Sanjeev
Mehta, G N
author_sort Ghosh, Samir
collection PubMed
description 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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spelling pubmed-28743122010-05-25 A short and efficient synthesis of valsartan via a Negishi reaction Ghosh, Samir Kumar, A Sanjeev Mehta, G N Beilstein J Org Chem Full Research Paper 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. Beilstein-Institut 2010-03-18 /pmc/articles/PMC2874312/ /pubmed/20502651 http://dx.doi.org/10.3762/bjoc.6.27 Text en Copyright © 2010, Ghosh et al. https://creativecommons.org/licenses/by/2.0https://www.beilstein-journals.org/bjoc/termsThis is an Open Access article under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The license is subject to the Beilstein Journal of Organic Chemistry terms and conditions: (https://www.beilstein-journals.org/bjoc/terms)
spellingShingle Full Research Paper
Ghosh, Samir
Kumar, A Sanjeev
Mehta, G N
A short and efficient synthesis of valsartan via a Negishi reaction
title A short and efficient synthesis of valsartan via a Negishi reaction
title_full A short and efficient synthesis of valsartan via a Negishi reaction
title_fullStr A short and efficient synthesis of valsartan via a Negishi reaction
title_full_unstemmed A short and efficient synthesis of valsartan via a Negishi reaction
title_short A short and efficient synthesis of valsartan via a Negishi reaction
title_sort short and efficient synthesis of valsartan via a negishi reaction
topic Full Research Paper
url 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
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AT ghoshsamir shortandefficientsynthesisofvalsartanviaanegishireaction
AT kumarasanjeev shortandefficientsynthesisofvalsartanviaanegishireaction
AT mehtagn shortandefficientsynthesisofvalsartanviaanegishireaction

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