title: A short and efficient synthesis of valsartan via a Negishi reaction.
abstract: 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.
authors.affiliation: Applied Chemistry Department, S.V. National Institute of Technology, Surat-395 007, India.
authors.forename: Samir
authors.initials: S
authors.lastname: Ghosh
authors.forename: A Sanjeev
authors.initials: AS
authors.lastname: Kumar
authors.forename: G N
authors.initials: GN
authors.lastname: Mehta