Abstract:Losartan was the oral non-peptide angiotensin Ⅱ receptor antagonist which was first approved by Sweden in 1994, and then approved by American Food and Drug Administration (FDA) in 2004. In recent years, Losartan has been the first-line antihypertensive drug. Structurally, Losartan was constituted by linking four structural fragment: imidazole ring (A), phenyl ring (B) and (C) as well as tetrazole ring (D). Based on the different linkage order of four ring fragment, the synthetic strategies of Losartan have been divided into five such as (B C) D A, (B C) A D, (C D) B A, (C D) (A B) and (A B) C D. In this paper, the progress in the synthetic process of Losartan has been reviewed from the perspective of five different synthetic strategies since its first discovery.