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 previously reported syntheses.
Ghosh
Samir
S
Applied Chemistry Department, S.V. National Institute of Technology, Surat-395 007, India.
Kumar
A Sanjeev
AS
Mehta
G N
GN