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A convenient method was developed for the preparation of thiolated compounds

In this work, based on the unique scaffold of indirubin, we synthesized 29 indirubin-3′-monoximes and preliminarily evaluated their antibacterial activities, especially against S. aureus.

An efficient radical synthesis of sulfurated oxindoles is developed using CoBr2 as both an initiator and a promoter. By controlling the CoBr2/(NH4)2S2O8 ratio, a wide range of sulfurated and brominated/sulfurated oxindoles are selectively prepared.

The overuse of antibiotics will led to the increase of drug resistance. Especially, the multidrug-resistant A. baumannii became the leading cause of nosocomial infections with high rates of morbimortality. The drug resistance of A. baumannii is greatly attributed to its biofilm. To alleviate the burden of drug resistance, the anti-virulence signaling strategies was developed. By specifically interfering with the ability of the bacteria to recognize host signals that are needed to establish infection, the bacteria are less able to colonize the host. In this paper, 39 N-acyl-2-aminopyrimidine derivatives were synthesized and tested for their biofilm inhibition efficacy. The screening results reveal that some of the analogues (3ac, 8d) efficiently inhibited the biofilm formation of A. baumannii (IC

An efficient aerobic iron-catalyzed annulation of unsaturated carboxylic acids with disulfides has been developed. This procedure proceeds using FeCl3 as the catalyst and KI as an iodine source under an air atmosphere, which provides practical access to a wide range of substituted γ-lactone derivatives. The disclosed method is quite simple, highly atom-economic, environmentally friendly, and tolerates a broad substrate scope.

A mild and efficient enantioselective amination of 4-alkylisoquinoline-1,3(2H,4H)-dione derivatives was established, which is compatible with a broad range of substrates and delivers the final products in excellent yields (up to 99%) and ee values (up to 99%) with low catalyst loading (down to 1 mol%). The synthetic potential of this methodology was also demonstrated in the gram scale level.

The first KI-catalyzed direct acyloxylation of indolin-3-ones with carboxylic acids has been developed using 30% aq. H2O2 as a green oxidant at room temperature. Through this strategy, various C2-acyloxy indolin-3-ones were obtained in up to 96% yield. Moreover, the C2-acyloxy indolin-3-ones can serve as versatile intermediates for the synthesis of nucleophilic 2-monoarylated indolin-3-ones and 3-ylidene indoles.

A highly enantioselective allylic alkylation of isoquinolinedione derivatives under palladium catalysis was developed in the preparation of quaternary carbon stereocenters. Under standard reaction conditions, excellent yields and enantioselectivities were realized and the products could be transformed into dihydroisoquinolone with vicinal chiral carbon centers or THIQ core structures in short steps with high yields.

A novel and efficient method for the synthesis of nucleophilic 2-monoarylated indole-3-ones via palladium-catalyzed direct C(sp3)–H arylation of indole-3-ones with aryl halides has been developed. Various 2-monoarylated indole-3-ones were readily obtained with yields up to 95%. As a class of important nucleophilic intermediates, 2-monoarylated indole-3-ones can be used for the construction of C2-quaternary indolin-3-one skeletons.

A palladium-catalyzed conia-ene reaction of 1-alkynylindolin-3-ones has been developed. Three examples of pyrrolo[1,2-a]indoline derivatives were readily obtained with yields up to 82% utilizing this strategy. Importantly, this palladium-catalyzed intramolecular cyclization process represents an important contribution to the application of indole-3-one derivatives.

An organocatalytic asymmetric α-sulfenylation of 2-substituted indolin-3-ones with N-(alkylthio or arylthio)succinimides has been developed for the first time using Cinchona-derived squaramide as the catalyst. Various chiral 2,2-disubstituted indole-3-ones with S- and N-containing heteroquaternary carbon stereocenters were obtained with up to 98% yield and 99% ee.

Base-catalyzed efficient hydroxylation of isoquinoline-1,3(2 H,4 H)-diones with air under transition-metal-free and reductant-free conditions was established. This methodology is essentially mild and compatible with a broad range of substrates, including aryl, heteroaryl, and alkyl groups. Also, the product could be simply transformed into a hydroxylated tetrahydroisoquinoline core structure through a reductive process.

A phosphine-catalyzed γ/γ-addition of oxindoles with allenoates has been developed that enables the efficient synthesis of highly functionalized symmetrical 3,3-disubstituted oxindoles. This protocol features mild reaction conditions and wide functional group tolerance and affording corresponding addition products in good to excellent yields. Besides, we have also investigated the biological utility of the typical 3,3-disubstituted oxindoles against nine phytopathogenic fungi, and 3a and 3d exhibited promising antifungal activities.

A novel and efficient method for the synthesis of nucleophilic 2-monoarylated indole-3-ones

Pentanidium catalyzed enantioselective 3-hydroperoxidation of 2-oxindoles with molecular oxygen has been established. Various 3-hydroperoxy-2-oxindoles were achieved in good ee and yield.