A highly efficient Rh‐catalyzed regioselective C8−H acylmethylation of quinoline N‐oxides with sulfoxonium ylides using N‐oxide as the directing group under air atmosphere has been developed. This transformation has the generality of a broad scope of substrates, avoids external oxidants, and provides an efficient protocol to C8−H acylmethylated quinolines.
A radical azidomethylation of various alkenes with azidotrimethylsilane and dimethyl sulfoxide has been achieved under mild reaction conditions, and the method efficiently introduces common and valuable azide and methyl groups into organic compounds. It offers a convenient method for preparing organic azides, which can be easily transformed into related amine derivatives and N-heterocycles. Control experiments such as capturing of the intermediate and gram-scale reactions of the developed system as well as further transformations of the products of the reaction are presented. And a free radical is involved in the reaction process.
A highly efficient phosphine-catalyzed [4+2] annulation of electron-deficient diene and alkyl vinyl ketone was developed for the first time, which provides an easy access to functionalized cyclohexenes. This method has the advantages of mild reaction conditions, widely functional group tolerance, high yields and transition metal free.
