Palladium-Catalyzed Coordination-Induced Remote C-H Aryl Etherification/Amination of 8-Amidoquinolines.

Herein, we report a direct method for palladium-catalyzed coordination-induced oxidative remote C-H aryl etherification of 8-amidoquinolines with -benzoquinone monoacetal. The method provides access to C5-aryl etherified quinolines and shows site-selectivity different from that of typical palladium-catalyzed C(sp)-H activation reactions. The -benzoquinone monoacetals act both as oxidants and as aryl etherification reagents.

Homologous Design and Three-Dimensional Quantitative Structure-Activity Relationship Study of Acaricidal 2,4-Diphenyloxazolines Containing Different Heteroatoms and Alkyl Chains.

In order to speculate the three-dimensional structure of the potential binding pocket of the chitin synthase inhibitor, a series of 2,4-diphenyloxazoline derivatives with different lengths of alkyl chains and heteroatoms were designed and synthesized by a homologous strategy. The bioassay results indicate that both the length of the alkyl chains and the type of substituents can affect the acaricidal activity against mite eggs. Compounds containing chloropropyl, alkoxyalkyl, and para-substituted phenoxyalkyl or phenylthioalkyl groups exhibit good activity, while those containing steric hindrance substituents or carbonyl substituents on the benzene ring exhibit reduced activity.

Design, Synthesis, Acaricidal Activities, and Structure-Activity Relationship Studies of Oxazolines Containing Ether Moieties.

To develop highly efficient and low cost acaricides, a series of 2,4-diphenyl-1,3-oxazolines containing an ether moiety at the position of the 4-phenyl group were synthesized from different alcohols and phenols. The bioassay results showed that most of the compounds, especially the short-chain alkyl ethers, exhibited excellent acaricidal activity against both the larvae and the eggs of . In particular, the -propyl ether compound possessed much better larvicidal activity (LC = 0.

Palladium Metallaphotoredox-Catalyzed 2-Arylation of Indole Derivatives.

Given that biaryl motifs are found in many useful molecules, including pesticides, pharmaceuticals, functional materials, and polymers, the development of methods for their construction is important. Herein, we report a two-step method for C(sp)-H/C(sp)-H cross-coupling reactions to synthesize 2-arylindole derivatives by combining palladium catalysis and photocatalysis. This mild, dual-catalysis method showed good functional group tolerance and a wide substrate scope and could be used for late-stage functionalization of oligopeptides, drugs, and natural products.

Diverse Oxidative C(sp)-N Bond Cleavages of Aromatic Fused Imidazoles for Synthesis of α-Ketoamides and N-(pyridin-2-yl)arylamides.

An efficient and chemoselective C(sp)-N bond cleavage of aromatic imidazo[1,2- a]pyridine molecules is developed. A broad scope of amide compounds such as α-ketoamides and N-(pyridin-2-yl)arylamides are afforded as the final products in up to quantitative yields. Diverse C-N bond cleavages are controlled by the oxidative species used in this transformation, with various amide products afforded in a chemoselective fashion.