TRANSITION-METAL-CATALYZED ALKYNE HYDROARYLATION WITH ARYLMETALS AND ARYL HALIDES

摘要

Arylalkenes are not only one of the most ubiquitous molecular scaffolds found in diverse natural products, materials, and pharmaceuticals, but they are also essential synthetic intermediates in both industrial and academic laboratories. Arylalkenescan be obtained by electrophilic aromatic substitutions, such as Friedel-Crafts acyla-tion, and subsequent functional group transformations to introduce the required sub-stituents on the alkenyl group. Such traditional preparative methods have fundamental disadvantages, such as the necessity of lengthy synthetic operations and the difficulty in the chemo- and site-selective introduction of substituents in the substituted aromatic precursors. The stereoselective construction of the tri- and tetrasubstituted alkene moieties is also a formidable challenge. Therefore, the development of a more straightforward and stereoselective method to prepare arylalkenes has been a particularly important objective in organic chemistry.