All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission Systemof respective journal.
Alternative synthesis of Valsartan via Negishi coupling
Author(s): Srinivas Ambati, Hanumantha Rao Penikelapati, T V Maruthikumar, Narahari Babu Ambati
A highly efficient approach to the synthesis of valsartan is described. Directed ortho-metalation of 4,4-dimethyl-2-phenyl-4,5-dihydrooxazole provides the key organozinc intermediate for palladium catalysed biaryl coupling with methyl N-(4-bromobenzyl)-N-pentanoyl-L-valinate (aryl bromide) obtained from alkylation of methyl N–pentanoyl-L-valinate. This methodology overcomes many of drawbacks associated with previously reported syntheses.