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
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands / M. Rabinowitz, P. Seneci, T. Rossi, M. Dal Cin, M. Deal, G. Terstappen. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 10:10(2000 May 15), pp. 1007-1010.
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands
P. SeneciSecondo
;
2000
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 throughputPubblicazioni consigliate
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