Solution-phase synthesis of an aminomethyl-substituted biaryl library via sequential amine N-alkylation and Suzuki cross-coupling.
Described herein is the semiautomated preparation of a 20-member aminomethyl-substituted biaryl library. The two-step solution-phase synthesis was achieved via sequential N-alkylation of various amines with either 3- or 4-bromobenzyl bromide and Suzuki cross-coupling of the resultant aryl bromides with various boronic acids.
Organ
M G
MG
Department of Chemistry, York University, 4700 Keele Street, Toronto M3J 1P3, Ontario, Canada.
Arvanitis
E A
EA
Dixon
C E
CE
Lavorato
D J
DJ
D000478:Alkylation; D057911:Angiotensin Receptor Antagonists; D001897:Boronic Acids / Q000138:chemical synthesis / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D007202:Indicators and Reagents; D019808:Losartan / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy
D057911:Angiotensin Receptor Antagonists; D001897:Boronic Acids; D007202:Indicators and Reagents; D019808:Losartan