ORGN 487 |
| Current pharmaceuticals access a miniscule 483 out of an estimated 10,000 druggable targets. Natural products are pre-designed and optimized in nature to interact with their protein targets and not surprisingly form the basis for 61% of 877 drugs introduced during the past two decades. Chemical proteomics, used to identify cellular targets of natural products requires the synthesis of natural product probes, where the choice of reactions for linker attachment is limited to hydrazone, ester and amide bond formation. We aim to expand the repertoire of reactions/functional groups available for conjugation and hasten the pace of finding new druggable targets. In this context, we have developed a highly selective rhodium catalyzed OH insertion/click chemistry sequence applicable to a broad range of polyhydroxy natural products. Influence of the substituents, the metal catalyst and emerging trends in reactivity of some of the OH groups encountered in natural products towards metal carbenoid species will be highlighted.
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Metal-Mediated Reactions and Syntheses
1:00 PM-5:00 PM, Wednesday, 29 March 2006 Georgia World Congress Center -- C302, Oral
Division of Organic Chemistry |
