Development of a Novel and Practical Synthesis of Angiotensin II Receptor Blockers by Means of C-H Bond Activation

Abstract

A highly efficient catalytic system for C-H bond activation has been developed which involves inexpensive ruthenium(II) chloride hydrate and a specific amount of triphenyl phosphine. The procedure has been successfully applied to a novel and practical synthesis of angiotensin II receptor blockers (ARBs). The residual ruthenium existed in the reaction mixture was thoroughly removed by the treatment with properly chosen metal scavengers. The new process permits a ready access to the important class of drugs in highly atom-economical and sustainable manner.