芳炔前体参与的芳烃1,2,3-三官能化反应

Aryne Precursors Participated 1,2,3-trifunctionalization of Aromatic Hydrocarbon

芳炔是一类重要的高活性反应中间体,由于它们可在芳环的相邻两个位置上同时实现不同基团的官能化,自发现以来已被广泛应用于有机合成化学中。传统单芳炔反应受到只能邻位双官能化的限制,无法有效发挥其在制备多取代芳环结构中的作用,目前国内外有关利用芳炔参与的的串联反应在芳环上一次性引入三个及以上官能团的报道非常少。文章综述了芳炔前体参与的芳烃1,2,3-三官能化反应及其在天然产物和药物的快捷合成方面的应用。

Arynes are a kind of important reaction intermediates with high activity.Since their discovery,they have been widely used in organic synthetic chemistry,because they can realize the functionalization of different groups at two adjacent positions of the aromatic ring at the same time.Limited to only ortho bifunctionalization,the traditional mono aryl alkyne reaction can not effectively play its role in the preparation of polysubstituted aromatic ring structures.At present,there are very few reports about the introduction of three or more functional groups into the aromatic ring at one time by using tandem reactions participated by arynes at home and abroad.1,2,3-trifunctionalization of aromatics involving aryl alkyne precursors and their applications in facile synthesis of natural products and pharmaceuticals were reviewed.