Arylation of Heterocycles via C-H Activation and Cross-Coupling with Aryl Chlorides

palladium - arylation - electron-rich heterocycles - aryl chlorides

Significance

<P>A new cheap and general method for the cross-coupling of heterocycles is presented in this article. A wide range of heterocycles was subjected to Pd-catalyzed C-H activation with subsequent cross-coupling to aryl and heteroaryl chlorides. This method was shown to be applicable to both electron-rich and electron-poor aryl chlorides furnishing good yields in almost all cases.</P>

Comment

<P>This new C-H activation-cross-coupling sequence has a very high practical value for the syntheses of biologically active compounds. A number of heterocycles are shown to be directly functionalizable by C-H activation. The possibility of their cross-coupling with the readily available aryl chlorides which are cheaper than their bromide or iodide equivalents is of considerable economic interest.</P>