Alkynes are widely present in natural products, biologically active molecules and organic functional materials. At the same time, they are also important intermediates in organic synthesis and can undergo abundant chemical transformation reactions. Therefore, the development of simple and efficient alkynes construction methods is particularly urgent and needed. Although the Sonogashira reaction catalyzed by transition metals is one of the most effective and convenient ways to synthesize aryl or alkenyl substituted alkynes, the coupling reaction involving non-activated alkyl electrophiles is due to side reactions such as bH elimination. Still full of challenges and less research, mainly limited to environmentally unfriendly and expensive halogenated alkanes. Therefore, the exploration and development of the Sonogashira reaction of new, inexpensive and easily available alkylation reagents will be of great significance both in laboratory synthesis and industrial applications. The team cleverly designed and developed a new, easily available and stable amide-type NN2 pincer ligand, which for the first time realized the efficient and high selection of alkylamine derivatives and terminal alkynes with a wide range of nickel catalytic sources, cheap and easy to obtain. The cross-coupling reaction has been successfully applied to the late deamination and alkynylation modification of complex natural products and drug molecules, which highlights the good reaction performance and functional group compatibility, and provides novelty for the synthesis of important alkyl-substituted alkynes. And practical methods.
Post time: Nov-22-2021