A short and efficient synthesis of valsartan via a Negishi reaction

Autor: Samir Ghosh, A. Sanjeev Kumar, G. N. Mehta
Jazyk: angličtina
Rok vydání: 2010
Předmět:
Zdroj: Beilstein Journal of Organic Chemistry, Vol 6, Iss 1, p 27 (2010)
Druh dokumentu: article
ISSN: 1860-5397
DOI: 10.3762/bjoc.6.27
Popis: 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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