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The use of high-throughput synthesis and purification in the preparation of a directed library of adrenergic agents
Authors:Siegel  Miles G  Shuker  Athony J  Droste  Christine A  Hahn  Patrick J  Jesudason  Cynthia D  McDonald III  John H  Matthews  Donald P  Rito  Christopher J  Thorpe  Andrew J
Institution:(1) Research Technology & Proteins Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN, 46285, U.S.A;(2) Endocrine Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN, 46285, U.S.A
Abstract: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 × 12 matrix, were combined to form 96 individual compounds. This revised version was published online in August 2006 with corrections to the Cover Date.
Keywords:adrenergic agonists and antagonists  ethanolamine library  ion exchange chromatography  parallel synthesis  reductive amination
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