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Phosphorus-based combinatorial libraries: Use of amino acid derivatives as synthons
Authors:Reza Fathi  Rina Patel  Alan F. Cook
Affiliation:(1) PharmaGenics Inc., 4 Pearl Court, 07401 Allendale, NJ, USA
Abstract:Summary Phosphorus has been used as a scaffold to prepare combinatorial libraries of phosphoramidates in which one of the diversity elements resulted from derivatives of amino acids. A small library was prepared for analytical and characterization purposes, followed by a larger library of approximately 8800 compounds. Libraries were assembled on solid supports using the conventional pool-and-divide method, followed by cleavage from the supports at the end of the synthesis. Mass spectrometry was used to confirm that library synthesis had been successful. Individual compounds were also prepared to study the stability of compounds of this type.
Keywords:Solid-phase synthesis  Combinatorial libraries  Phosphoramidate  Amino acid
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