A5100669059- Catalytic C–H Functionalization Methods
- Synthesis and Catalytic Reactions
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Analysis
- Asymmetric Hydrogenation and Catalysis
- Synthesis and Biological Evaluation
- Energy Efficiency and Management
- Phagocytosis and Immune Regulation
- Metal-Catalyzed Oxygenation Mechanisms
- Housing Market and Economics
- Click Chemistry and Applications
- Liver Diseases and Immunity
- Pancreatic and Hepatic Oncology Research
- CO2 Reduction Techniques and Catalysts
- Capital Investment and Risk Analysis
- Oxidative Organic Chemistry Reactions
- Cancer Mechanisms and Therapy
- Drug Transport and Resistance Mechanisms
- Catalytic Alkyne Reactions
- Alkaloids: synthesis and pharmacology
- Carbon dioxide utilization in catalysis
- Chemical synthesis and alkaloids
- Asymmetric Synthesis and Catalysis
- Liver Disease Diagnosis and Treatment
Institute for Advanced Study
2025
University of Chinese Academy of Sciences
2025
Shanghai Institute of Materia Medica
2018-2025
Chinese Academy of Sciences
2018-2025
Nanjing University of Chinese Medicine
2020-2023
Huaibei Normal University
2021
Shanghai University
2017-2018
Abstract Rhodium(III)‐Catalyzed C−H activation of benzoylacetonitriles in coupling with sulfoxonium ylides was developed to synthesize diversified substituted naphthols, which aryl, heterocyclic and alkyl groups are tolerated. Intriguingly, we have further implemented transformation for 1‐naphthols give some intriguing fused tricyclic compounds derivatives propranolol, demonstrate the practical utility this methodology. magnified image
A chemical method for the preparation of nonprotected tryptophan via nickel(II) complexes under simple operating conditions was established. The carefully designed glycinates are inexpensive and can be quantitatively recovered releasing target tryptophans in high yield. has a wide range synthesis generality, allowing various substituted tryptophans. Furthermore, scalability this bodes well its synthetic use as general approach to biologically interesting tailor-made related compounds.
Rh (III)-catalyzed C–H activation of benzoylacetonitriles in coupling with diazo compounds was developed to synthesize diversified substituted benzo[de]chromenes via a formal (4 + 2) cycloaddition compound and subsequent tandem another compound. Intriguingly, synthesis their decarboxylation products could be realized by controlling the reaction conditions. These reactions have broad range substrates, moderate good yields, high regioselectivity.
In the present study, a novel synthetic strategy to directly produce versatile 3-acylindoles through Rh(III)-catalyzed C-H activation and annulation cascade of N-phenylamidines with α-Cl ketones was developed, in which serve as unusual one-carbon (sp3) synthons. This features high regioselectivity, efficiency, wide substrate tolerance, mild reaction conditions, further underscore its utility drug molecule synthesis.
Recently, N-hydroxyindole derivatives have received much interest because of their unique structural motif and various biological activities. In this study, we report the first example a Rh(III)-catalyzed reaction arylnitrones with α-diazoketoesters or α-diazodiketones to produce derivatives. Intriguingly, could build scaffold by blocking cleavage N–O bond selectively, while eliminating acyl group preferentially.
Here, we report a novel strategy for constructing maleimide-containing peptides and cyclic using Rh(III)-catalyzed tryptophan (Trp) (C7) alkenylation, which is challenging due to the inherent reactivity of indole benzenoid ring. This method scalable exhibits broad substrate scope. The utility this protocol could further be demonstrated by synthesis peptide conjugates with natural products amino acids as well construction maleimide-braced peptides.
Here, we report on methods for late-stage peptide diversification through palladium-catalyzed site-selective C(sp2)–H amination of tryptophan residues at the C4 position, utilizing tryptophan-amine cross-links. Our strategy enables practical access to C–N bonds, facilitating construction cyclopeptides via cyclodimerization structurally complex peptides, which poses significant challenges organic synthesis. The synthetic utility this protocol is demonstrated synthesis 30- 38-membered...
We herein report the synthesis of substituted tryptophans using Ni(II) complexes glycine and gramines. This reaction proceeds under operationally convenient mild conditions, inexpensive, nontoxic, easily accessible reagents. The reactions feature high yields virtually complete thermodynamically controlled diastereoselectivity, providing a method for tailor-made tryptophans.
We here described a method to synthesize α-keto amides from simple sulfoxonium ylides and secondary amines under the catalysis of copper. This transformation involved very clean catalytic system, substrates could be extended aryl, heteroaryl, tert-butyl give diversified with good yields. Additionally, mechanistic studies indicated that α-carbonyl aldehyde might key intermediate in reaction system.
Farnesoid X receptor (FXR) plays a key role in bile acid homeostasis, inflammation, fibrosis, and metabolism of lipid glucose becomes promising therapeutic target for nonalcoholic steatohepatitis (NASH) or other FXR-dependent diseases. The phase III trial results obeticholic demonstrate that the FXR agonists emerge as intervention patients with NASH but this acid-derived agonist brings severe pruritus an elevated risk cardiovascular disease patients. Herein, we reported our efforts discovery...
Rh(III) catalysts have played increasingly important roles in the activation of C–H bonds to build heterocyclic scaffolds. However, there are few reports on more challenging synthesis pharmaceutically 2H-isoindoles and fused 2H-isoindoles. The process reported herein is an effective strategy produce 2H-isoindole or derivatives via a Rh(III)-catalyzed transformation α-iminonitriles α-imino esters with acrylates.
As a novel and promising antitumor target, AXL plays an important role in tumor growth, metastasis, immunosuppression drug resistance of various malignancies, which has attracted extensive research interest recent years. In this study, by employing the structure-based design bioisosterism strategies, we designed synthesized total 54 inhibitors featuring fused-pyrazolone carboxamide scaffold, up to 20 compounds exhibited excellent kinase BaF3/TEL-AXL cell viability inhibitions. Notably,...
Multiple-spiro/fused-heterocyclic frameworks containing indazolone are structurally unique and represent a class of potentially dominant skeletons. In this work, we successfully fulfilled Rh(III)-catalyst mediated substrate- pH- controlled strategies to construct four novel types complicated penta-spiro/fused-heterocyclic via C-H activation/[4+1] [4+2] annulation cascades. This method had mild reaction conditions, broad scope substrates, moderate good yields, valuable applications, which...
The spiroindolenine framework is a privileged heterocyclic motif and widely present in numerous indole alkaloids.
Abstract Invited for the cover of this issue are Xuewu Liang, Hong Liu and co‐workers at Shanghai Institute Materia Medica Shenyang Pharmaceutical University. The image depicts how a rhodium‐catalyzed methodology leads to novel penta‐spiro/fused‐heterocyclic frameworks with potent antitumor activity through C−H activation/[4+1] [4+2] annulation cascades. Read full text article 10.1002/chem. 202301553 .
To explore alternative approaches to the CO2 reduction formate and provide an insight into spin state effect on reduction, we theoretically designed a kind of low-valence iron(I) model complex, whose doublet, quartet, sextet states are denoted as 2Fe(I), 4Fe(I), 6Fe(I), respectively. This complex is featured with center, which bonds 1,2-ethanediamine (en) 2-hydroxy-biphenyl group. Reaction mechanisms for catalyzed by this were explored using density functional theory (DFT) computations....