| Alkynes and their derivatives are important structural moieties and general synthesizer that are widely used in material chemistry,biochemistry and organic synthesis chemistry.Therefore,enormous efforts have been devoted to effective synthesis of alkynes.The most classical synthesis method of alkynes is the combination of aryl chloride and terminal alkynes via Sonogashira coupling.However,this method not only requires the pre-functionalization of aromatic substrates,but also the self-dimerization of terminal alkynes.Over the past several decades,great progress has been made in the study of C-H alkynylation of aromatic substrates using TIPS-EBX,which is not easy to dimerize,but the regioselective activation of specific C-H remains a great challenge.In this paper,1-phenyl-5-pyrazolone was selected as aromatic substrates and[Cp*RhCl2]2 and AuCl were used as catalysts to achieve regioselective alkynylation by C-H activation.Considering from the point of view of synthesis methodology,1-phenyl-5-pyrazolone have reactivity at the ortho-and heterocyclic C-4 positions of the benzene ring.Therefore,we can achieve regioselective alkynylation by selectively control.On the other hand,1-arylpyrazolones play a key role in the synthesis of bioactive molecules and natural products.When the R group is H atom,under the catalysis of Rh（III）,the alkynylation occurred at the aryl ring with the assistance of an N-chelation group.When the R group is methyl,the Au-catalyzed C4-selective alkynylation of pyrazolones proceeded via an electrophilic pathway. |
