Pd(<scp>ii</scp>)-catalyzed, controllable C–H mono-/diarylation of aryl tetrazoles: concise synthesis of Losartan

Abstract

A palladium(II)-catalyzed C-H arylation directed by tetrazole, a metabolically stable surrogate for the carboxylic acid group in drug design, has been developed. Excellent mono-/di-selectivity was achieved through adjustment of the protecting site on the tetrazole ring. The synthetic utility of this new transformation was demonstrated in the concise total synthesis of Losartan.