Improved Synthesis of Valsartan via Nucleophilic Aromatic Substitution on Aryloxazoline

Abstract

A highly efficient approach to the synthesis of the angiotensin II receptor antagonist valsartan (Diovan), one of the most important agents used in antihypertensive therapy today is described. The formation of the aryl–aryl bond represents the key step of its synthesis, which has been done by simple nucleophelic aromatic substitution on aryloxazoline with good yield and purity.

Keywords:

• Antihypertensive therapy
• nucleophilic aromatic substitution
• oxazoline
• valsartan

ACKNOWLEDGMENTS

We are grateful for the support of the Sardar Vallabhbhai National Institute of Technology Surat and Indian Association for the Cultivation of Science, Jadhavpur, India.