Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands |
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Authors: | Rabinowitz M Seneci P Rossi T Dal Cin M Deal M Terstappen G |
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Affiliation: | Glaxo Wellcome, Inc., Research Triangle Park, NC 27709, USA. mhr20812@glaxowellcome.com |
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Abstract: | A novel solid-phase/solution-phase strategy for the synthesis of neuroimmunophilin ligands based on GPI 1046 was developed. The synthesis employs a solid-phase esterification strategy followed by a solution-phase pyruvic amide formation to produce multi-milligram quantities of discrete compounds for assay. The protocol was applied to a production library of 880 discrete compounds. A highlight of the strategy is an aqueous extractive purification of the final compounds using a novel liquid/ice extraction system developed for high throughput. |
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