Facile synthesis of novel nonpeptide angiotensin II receptor antagonists

✍ Scribed by Ling-Chun Yang; Guan-Xin Zhang; Nan-Zhi Zou; Chuan-Min Qi

• Book ID: 102341923
• Publisher: Journal of Heterocyclic Chemistry
• Year: 2003
• Tongue: English
• Weight: 65 KB
• Volume: 40
• Category: Article
• ISSN: 0022-152X
• DOI: 10.1002/jhet.5570400623

✦ Synopsis

Abstract

A series of Losartan analogues 1‐12 with different functional groups were synthesized and characterized. In comparison with the previous reports, the synthetic procedures described in this paper have been optimized as follows below: 1) preparation of aromatic amine 15 and 18 through hydrogenation by employing Raney Ni and hydrazine as catalysts in place of palladium; 2) preparation of nitro‐compound 17 by using pure fuming nitric acid at ‐20 ‐ ‐15 °C; 3) alkylation of 21 with 22 or 23 in the presence of sodium hydride in place of potassium tert‐butylate; 4) preparation of carboxylic acid 4 by ester cleavage rather than hydrolysis of cyano group.