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Paper | Special issue | Vol 39, No. 1, 1994, pp.117-131
Published online, 1st January, 1970
DOI: 10.3987/COM-93-S(B)5
Synthesis of 7-Ethyl-1,2-dihydroquinolin-2-ones as Angiotensin II Receptor Antagonists

Norbert Beier, Erwin Labitzke, Werner W.K.R. Mederski,* Hans-Eckart Radunz, Karin Rauschenbach-Ruess, and Björn Schneider

*E. Merck, Preclinical Pharmaceutical Research Laboratories, 64271 Darmstadt, Germany


A number of biphenyl substituted 1,2-dihydroquinolin-2-ones were synthesized by regiospecific alkylation of the corresponding 1H-derivatives. Again, these precursors were prepared in three steps by acetoacetylation of anilines, regiospecific C-alkylation of the resulting β-ketoanilides and subsequent condensation to the quinolinones. One of the target compounds, 2-[7-ethyI-4-methyl-2-oxo-1-[(2’-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-1,2-dihydroquinolin-3-yl]-N,N-dimethylacetamide (10e), is a potent angiotensin II receptor antagonist.