ORGN 584 |
Enhancing the screening collection with drug-like developable molecules is a key goal for high throughput chemistry groups. Toward this end, an efficient methodology for the solid-phase parallel synthesis of aminocarbonylbenzenesulfonamides has been developed. Using high-loading 2,6-dimethoxy-4-polystyrenebenzyloxy-benzaldehyde (DMHB) resin, a 5,184-member array was prepared in high purity and yield via a six-step sequence. The solid-phase reaction conditions were fully optimized and a variety of amines and aldehydes were scanned and used during array production. A large percentage of the compounds prepared could directly be registered and submitted for biological screens without purification. The reaction details, chemistry platform and analytical results will be described.
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Asymmetric Reactions, Heterocycles, Aromatics, Combinatorial, and Physical Organic Chemistry
8:00 PM-10:00 PM, Wednesday, 31 August 2005 Washington DC Convention Center -- Hall A, Poster
Division of Organic Chemistry |