A general preparation of (Z)-1-fluorostilbene derivatives for the design of conformationally restricted peptidomimetics

作者：Williams David R^*; Fultz Micheal W; Christos Thomas E; Carter Jeffery S

来源：Tetrahedron Letters, 2010, 51(1): 121-124.

DOI：10.1016/j.tetlet.2009.10.099

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.

• 出版日期2010-1-6