Biaryl Units in Valsartan and Vancomycin

Biological target Valsartan is a non-peptide, biaryl antagonist at the angiotensin 11 type 1 (ATI), G-protein-coupled receptor. It, therefore, blocks the stimulation of vasoconstriction, aldosterone release and salt retention by the kidney, leading to a fall in blood pressure. 

Vancomycin is a glycopeptide antibiotic originally isolated from Streptomyces orientalis. It blocks the formation of the bacterial cell wall protein murein by forming a complex with o-alanyl-o-alanine. 

Therapeutic profile Valsartan is a leading dmg for the treatment of hypertension. 

Vancomycin is a broad spectrum antibiotic, administered intravenously for the treatment of Gram-positive bacterial infections resistant to other antibacterials. 

Synthetic highlights The Cu-promoted catalytic decarboxylative, biaryl synthesis of valsartan is an example of biomimetic, aerobic decarboxylation and enables C-C bond formation in aqueous solution. The chiral variant of biaryl synthesis is exemplified by the stereoselective approach to the axially chiral biaryl system present in vancomycin. 

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