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.
Y. Ding, Y. Li, S. Dai, Q. Lan and X. Wang, Org. Biomol. Chem., 2015, 13, 3198 DOI: 10.1039/C4OB02453B
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