Journal
ACS COMBINATORIAL SCIENCE
Volume 15, Issue 9, Pages 503-511Publisher
AMER CHEMICAL SOC
DOI: 10.1021/co400078r
Keywords
drug discovery; drug-likeness; lead-likeness; computational library design; library synthesis; continuous flow hydrogenation; enabling technologies; aminopiperidines
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A platform that incorporates computational library design, parallel solution-phase synthesis, continuous flow hydrogenation, and automated high throughput purification and reformatting technologies was applied to the production of a 120-member library of 1-aryl-4-amino-piperidine analogues for drug discovery screening. The application described herein demonstrates the advantages of computational library design coupled with a flexible, modular approach to library synthesis. The enabling technologies described can be readily adopted by the traditional medicinal chemist without extensive training and lengthy process development times.
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