Transition Metal Catalyzed Direct C-2 Alkynylation Of Indole

This thesis investigated,palladium-catalyzed direct C2 alkynylation of N-2-pyrimidyl indoles,affording a series of C2 alkynylated indole derivatives in good yields.In addition we developed the direct alkynylation of 3-methyl-2-phenylpyridine.The main contents are outlined as follows:Indole derivatives are a kind of organic heterocyclic compounds with physiological activity and important drug intermediates.As a parent,nuclear structure is commonly used in anticancer drugs with high activity,and N-pyrimidine indole is used as substrate.Herein,a palladium-catalyzed direct C2 alkynylation of N-2-pyrimidyl indoles was described by using 2-Bromo-l-triisopropylsilyl acetylene as an alkyne reagents.This reaction exhibited excellent regioselectivity of indoles by using the pyrimidine moiety as the directing group,and the desired mono-substituted alkynylated products were obtained in high yields.This reaction proceeded smoothly under the following given conditions and showed good functional group compatibility as shown in Figure 0.1.Figure 0.1 Direct C2 alkynylation of N-2-pyrimidyl indole...