883223-07-2

Upstream product

• 87268-78-8 2-trityl-5-phenyl-2H-tetrazole 
• 76-83-5 trityl chloride 
• 73096-42-1 5-(2-bromophenyl)-2H-tetrazole 
• 2042-37-7 o-cyanobromobenzene 

Downstream Products

• 137862-53-4 N-pentanoyl-N-[[2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]-methyl]-(L)-valine 
• 137863-17-3 methyl N-((2’-(1H-tetrazol-5-yl)-[1,1’-biphenyl]-4-yl)methyl)-N-pentanoyl-L-valinate 

Relevant academic research and scientific papers

Efficient synthesis of valsartan, a nonpeptide angiotensin II receptor antagonist

A highly efficient and convergent approach to the synthesis of the angiotensin II receptor antagonist valsartan (1), one of the most important agents used in antihypertensive therapy today, is described. Directed ortho-metalation of 4-bromotoluene provides the key boronic acid intermediate 11 which was subjected to palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses. The saponification of the methyl ester in valsartan was realized in a convenient and economical manner, which is more suitable for industrial production. Georg Thieme Verlag Stuttgart.

On the relative strength of the 1H-tetrazol-5-yl- and the 2-(triphenylmethyl)-2H-tetrazol-5-yl-group in directed ortho-lithiation

ortho-Lithiation followed by electrophilic trapping of N-unsubstituted and N2-triphenylmethyl substituted 5-aryltetrazoles, further substituted with another ortho-director at the para position of the aryl ring, resulted in the formation of regioisomers of