Improved Methods for the Synthesis of Irbesartan, an Antihypertensive Active Pharmaceutical Ingredient

Abstract

New methods for the preparation of irbesartan 1 have been described. The dehydration and tetrazole formation in one step from substituted cyclopentane derivative 7 with tributyltin chloride and sodium azide is described. Selective hydrolysis of nitrile 3 with HCl has also been described in the preparation of N‐acylaminocyclopentane‐2‐carboxylic acid 4, which is the key intermediate for the preparation of irbesartan. The impurity profiling of irbesartan has also been discussed.

Keywords:

• antihypertensive drug
• impurities
• irbesartan
• synthesis

Acknowledgment

The authors thank the management of Aurobindo Pharma ltd., Research and Development Department, for supporting this work. The authors also thank the Analytical Research Department for its valuable contribution to this work.