The combination of ArB(OH)2 transmetallation with cationic gold(I) [LAu]+ and electrochemical anodic oxidation (EAO) approach was successfully developed for the preparation of AuIII-Ar intermediate for the first time. This in-situ generated aryl gold intermediate gave rapid and controllable transmetallation with ArB(OH)2 or alkyne followed by reductive elimination to generate either di-aryl coupling

A convenient method for the rapid construction of indolo[2,3-b]indoles has been developed. This cascade reaction involving condensation, dehydroaromatization, and oxidative annulation was achieved in a one-pot TMSI/DMSO system, providing a diversity of functionalized indolo[2,3-b]indoles in satisfactory yields under facile metal-free conditions. The present protocol provides a straightforward approach

A four-component and one-pot synthesis involving N,S-acetalation of aldehydes with cysteine followed by the reaction with second aldehydes for decarboxylative [3 ?+ ?2] cycloaddition with maleimides is developed for stereoselective synthesis of tetrahydropyrrolothiazoles. High synthetic efficiency, using EtOH as solvent and catalyst, and only releasing CO2 and H2O as byproducts make this method favorable

Isoindolinone- and tetrahydroisoquinoline-based cyclic scaffolds comprise the key, structural feature of a wide range of biologically active molecules. Here we report an, approach for the synthesis of chiral isoindolinones and tetrahydroisoquinolines based, on the umpolung allylation of imines. The products contain a free N–H group, which is, primed for further derivatization.

A manganese/NaOPh co-catalyzed C2-selective C–H conjugate addition of indoles to α,β-unsaturated carbonyls has been developed. The reaction features very high atom economy in which no stoichiometric reagents/additives were employed. The crucial role of sodium phenolate (NaOPh) as a synergetic catalyst was revealed in the reaction screening process and mechanistic experiments.

An efficient procedure to access to ortho-SCF3 substituted benzophenones from arynes and trifluoromethylthioesters has been developed under transition-metal free conditions. This difunctionalization process involves the first insertion of arynes into the C–S σ-bonds to achieve vicinal trifluoromethylthiolation-acylation of arenes in one step.

A novel approach was developed for the synthesis of 5H-isochromeno [4,3-b]indolizin-5-ones (ICIDOs) 3 through a cascade reaction of 1,2,3-indantriones 1 with ethyl 2-(pyridine-2-yl)acetates 2. Various 5H-isochromeno [4,3-b]indolizin-5-ones were produced by heating of the mixture of 1,2,3-indantriones and ethyl 2-(pyridine-2-yl)acetates for approximately 8 ?h in an environmentally-friendly PEG200 solvent

Regioselective syntheses of glycosides using modern chemical methods suffer from the need to invoke multiple steps of protection and deprotection, and even then product mixtures may occur. Discovering and tuning by mutagenesis glycosyltransferases (GTs) with considerable substrate promiscuity is an alternative challenge. We tuned by rational design based on extended Focused Rational Iterative Site-specific

We constructed an advanced MnO2 catalyst with abundant OVs through interstitial nitrogen doping. When used in the oxidation of p-methyl benzyl alcohol to p-methyl benzyl aldehyde, the N1.8-MnO2-300 catalyst gave a 94.7% yield of the desired product at 30 ?°C, with excellent recyclability.

Two highly efficient artificial light-harvesting systems have been successfully constructed in aqueous solution, which can be used as supramolecular nanoreactors for efficient photocatalysis.

Owing to their importance in organic synthesis, transition metal catalyzed cross-coupling reactions have been the focus of many studies. Recently, it was recognized that merged transition metal and photoredox catalysis is a powerful strategy for the design of challenging Csp3–Csp2 bond forming cross coupling reactions. However, these reactions require metals (e.g., Ni) to activate Csp2-halogen bonds

As one of the most important biogeochemical cycles, the carbon dioxide (CO2) cycle between atmosphere and biosphere has a profound impact on the life on earth. Therefore, the search for sustainable solutions to normalize the currently unbalanced carbon dioxide cycle is the central research topic of many scientific disciplines. The green and sustainable electrocatalysis offers a very promising answer

P-stereogenic compounds are an important class of compounds with unique chemical properties, which play important roles in various fi elds such as medicine, pesticides, and organometallics. Methods to obtain optically pure phosphorus compounds effi ciently are a core issue. Rigorous research has been conducted in recent years and many highly effi cient and green strategies have emerged to prepare such

A protein engineering strategy based on Focused Rational Iterative Site-specifi c Mutagenesis (FRISM) was developed in order to evolve mutants that allow for the fi rst time the glucosylation of polyhydroxy substrates such as silybin ( 1 ) with essentially complete regioselectivity, leading to the synthesis of pharmaceutically interesting products 2 , 3 and 4 , respectively. This approach also enables

Chiral benzylic boronic esters were synthesized through a simple three-component reaction involving a terminal alkene, an aryl bromide and B2pin2?using a nickel catalyst. Interestingly, the reaction yielded a 1,1-difunctionalized alkane instead of a 1,2-difunctionalized product. Mechanistic investigations supported a 1,2-Ni migration to achieve the 1,1-difunctionalized product. The 1,1-addition addition

An efficient and practical synthetic approach was developed for the tandem synthesis of trisubstituted 2-pyrone derivatives from sulfoxonium ylides and cyclopropenones. This [3?3] annulation reaction was carried out under transition-metal-free conditions. A broad range of functional groups were tolerant under mild conditions, and a variety of 2-pyrones were obtained in moderate to good yields.

A ruthenium-catalyzed electrochemical dehydrogenative C(sp2) H acyloxylation of aniline derivatives with carboxylic acids has been developed. Electric current is used to recycle the active ruthenium-based catalyst and promote H2 evolution. This method significantly expands the scope and enhances the selectivity of metal-electron catalyzed mono- and di-acyloxylations, which remain challenged. Our findings

Transition-metal-catalyzed direct C¨CH/C¨CH cross-coupling reactions as efficient and atom-economical approaches have been widely used to build up complex heterocyclic compounds. However, the strategy for preparation of biphenyl-2-carbonitriles has not been well established. Herein, we described the first cyanogen directed Rh(III)- catalyzed CDC reaction of aromatic nitriles with heteroarenes. Various

Both O-glycosides and nucleosides are essential biomolecules with important roles in a variety of biological processes. Chemical synthesis of both O-glycosides and nucleosides is a scalable and reliable method to develop new therapeutic agents and decipher their functions. However, the efficient synthesis of both O-glycosides and nucleosides remains one of long-standing challenges in chemical synthesis