Ruthenium(â…¡)-Catalyzed Direct C-H Alkynylation Of N-pyrimidine Indoles

In this thesis, ruthenium-catalyzed diredct C2 alkynylation of N-pyrimidine indoles was investigated, affording a series of C2 alkynylated indole derivatives in high yields. The main contents are outlined as follows:Indole uinits are importent intermediates in various organic heterocyclic compounds and parmeceuticals. Herein, a ruthenium-catalyzed diredct C2 alkynylation of N-pyrimidine indoles was described by using triisopropylsilylethynyl-1,2-benziodoxol-3(1H)-one as an alkyne reagents. This reaction exhibited excellent regioselectivity of indoles by using the pyrimidine moiety as the diredcting group, and the desired mono-substituted alkynylated products were obtained in high yields. This reaction proceeded smoothly under mild conditions and showed good functional group compatibility(Scheme 1).