A general preparation of (Z)-1-fluorostilbene derivatives for the design of conformationally restricted peptidomimetics |
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| Authors: | David R. Williams Micheal W. Fultz Jeffery S. Carter |
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| Affiliation: | a Department of Chemistry, Indiana University, Bloomington, IN 47405, USA
b Icagen, Incorporated, Research Triangle Park, NC 27709, USA |
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| Abstract: | The preparation of (Z)-1-fluoro-2-bromostyrenes provides a general route for the formation of (Z)-1-fluorostilbene derivatives as configurationally stable spacial linkers for the design of conformationally restricted peptidomimetics. Palladium-catalyzed aryl Suzuki and Stille cross-coupling reactions have been surveyed to proceed with complete retention of fluoroalkene geometry, and permit the direct incorporation of a variety of aryl and heteroaromatic substituents. |
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