With sunlight or blue LEDs irradiation, regioselective decarboxylative alkylation of various non-aromatic heterocycles has been realized via C (sp 3 )-centered radical C(sp 2 )À C(sp 3 ) bond formation under oxidant-free conditions at room temperature. This reaction readily incorporates various functional alkyl groups into heterocyclic compounds without observation of any alkyl radical rearrangement and represents a mild and general tool for the preparation of valuable alkyl group-functionalized heterocyclic compounds.

A facile, general, and economical synthesis of diversely functionalized pyrimidines has been realized under basic conditions via the copper-catalyzed cyclization of ketones with nitriles. The reaction proceeds via a novel pathway involving the nitriles acting as electrophiles and consecutive C-C bond and two C-N bond formations and shows broad substrate scope and good tolerance of many important functional groups. This strategy represents a new platform for constructing pyrimidine structures.

The cyclization−coupling reaction of 2-bromoaryl ketones and terminal alkynes is first realized by copper catalysis, which produces polyfunctional naphthyl aryl ethers in moderate to excellent yields with broad substrate scope and good functional group tolerance. This reaction proceeds via 6-endo-dig cyclization and C(sp 2 )−O coupling using green H 2 O as the unique solvent and 5-bromopyrimidin-2-amine as the critical additive. Mechanistically, a unique Cu(III)-acetylide probably is the key intermediate, which allows exclusive 6-endo-dig selectivity.N aphthyl aryl ethers are an important class of structural motifs found in natural products, bioactive molecules, and functional materials. 1,2 For example, naphthyl aryl ether derivatives I−V are known as a potential anticancer agent, an antimalaria agent, a BRCA1 inhibitor, and an MEK inhibitor, as well as an organo-electronic element (Figure 1). However,