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Bioorg Med Chem Lett. 2000 May 15;10(10):1007-10.

Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.

Author information

1
Glaxo Wellcome, Inc., Research Triangle Park, NC 27709, USA. mhr20812@glaxowellcome.com

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.

PMID:
10843203
DOI:
10.1016/s0960-894x(00)00104-9
[Indexed for MEDLINE]

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