The use of high-throughput synthesis and purification in the preparation of a directed library of adrenergic agents.
A library of potential agonists and antagonists for adrenergic receptors was prepared using high-throughput solution-phase parallel synthesis. Traditional solution-phase reductive amination reactions followed by rapid purification by ion exchange chromatography yielded products with near-analytical purity. An array of ketones and amines, arranged in an 8 x 12 matrix, were combined to form 96 individual compounds.
Siegel
M G
MG
Research Technology & Proteins, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA.
Shuker
A J
AJ
Droste
C A
CA
Hahn
P J
PJ
Jesudason
C D
CD
McDonald
J H
JH
Matthews
D P
DP
Rito
C J
CJ
Thorpe
A J
AJ
D000322:Adrenergic Agonists / Q000138:chemical synthesis*; D018674:Adrenergic Antagonists / Q000138:chemical synthesis*; D000588:Amines / Q000737:chemistry; D002852:Chromatography, Ion Exchange; D004983:Ethanolamines / Q000138:chemical synthesis; D007659:Ketones / Q000737:chemistry; D015394:Molecular Structure; D011941:Receptors, Adrenergic / Q000378:metabolism
D000322:Adrenergic Agonists; D018674:Adrenergic Antagonists; D000588:Amines; D004983:Ethanolamines; D007659:Ketones; D011941:Receptors, Adrenergic