Pd‐Catalyzed Cyclization of Alkynyl Norbornene Derivatives for the Synthesis of Benzofused Heteroarenes
作者:Hayeon Kwak、Eunsu Kang、Jae Yeong Song、Geunhee Kang、Jung Min Joo
DOI:10.1002/adsc.202100763
日期:2021.11.9
Modular approaches, which allow a systematic variation of heteroaromatic cores and substituents, are crucial for the development of heteroaromatic drug candidates and organic functional materials. A new strategy involving the cyclization of heteroarenes tethered with alkynes through a norbornene bridge was developed. The precursors were readily prepared by a three-component coupling process of heteroaryl
An inexpensive BF3·Et2O-catalyzed annulation reaction of arylacetaldehydes with arylalkynes has been developed. Various substituted phenylacetaldehydes and phenylacetylenes can undergo this reaction, producing corresponding α-aryl substituted naphthalenederivatives. Use of inexpensive and readily available BF3·Et2O catalyst constitutes the most attractive advantage of this transformation.