Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands
| Autor: | Martyn Deal, T. Rossi, Georg Terstappen, Michael H. Rabinowitz, Pierfausto Seneci, Michele Dal Cin |
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| Rok vydání: | 2000 |
| Předmět: |
Pyrrolidines
Aqueous solution Combinatorial Chemistry Techniques Chemistry Organic Chemistry Clinical Biochemistry Extraction (chemistry) Pharmaceutical Science Ligands Combinatorial synthesis Biochemistry Solution phase Combinatorial chemistry Tacrolimus Binding Proteins chemistry.chemical_compound Phase (matter) Amide Drug Discovery Molecular Medicine Immunophilins Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 10:1007-1010 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)00104-9 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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