A5026097306- Catalytic C–H Functionalization Methods
- Asymmetric Synthesis and Catalysis
- Asymmetric Hydrogenation and Catalysis
- Synthesis and Catalytic Reactions
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Sulfur-Based Synthesis Techniques
- Catalytic Cross-Coupling Reactions
- Oxidative Organic Chemistry Reactions
- Axial and Atropisomeric Chirality Synthesis
- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Synthesis of Indole Derivatives
- Chemical Synthesis and Reactions
- Radical Photochemical Reactions
- Synthesis and Characterization of Pyrroles
- Cyclopropane Reaction Mechanisms
- Peroxisome Proliferator-Activated Receptors
- Advanced oxidation water treatment
- Carbon dioxide utilization in catalysis
- Molecular spectroscopy and chirality
- Bioactive Compounds and Antitumor Agents
- Chemical synthesis and alkaloids
- Crystallography and molecular interactions
- Synthesis and Biological Evaluation
China Pharmaceutical University
2015-2025
State Key Laboratory of Natural Medicine
2015-2025
Southeast University
2018-2020
Shanghai Pulmonary Hospital
2019
Huazhong Agricultural University
2016-2017
Chinese Academy of Sciences
2010-2016
Shanghai Institute of Organic Chemistry
2010-2016
Nanjing Agricultural University
2016
Rice University
2015-2016
Ningbo First Hospital
2015
Abstract We disclose an efficient and operationally simple protocol for the preparation of fused N‐heterocycles starting from readily available 2‐nitrobiaryls PhMgBr under mild conditions. More than two dozen N‐heterocycles, including bioactive natural products, have been synthesized using this method. A stepwise electrophilic aromatic cyclization mechanism was proposed by DFT calculations.
The cyclic GMP-AMP synthase (cGAS)-stimulator of the interferon genes (STING) pathway plays a key role in triggering and inflammatory responses against microbial invasion or tumor. However, aberrant activation cGAS-STING is associated with variety autoimmune diseases, thus inhibition STING regarded as potential new approach to treating these diseases. Herein, we report series novel indolyl-urea derivatives inhibitors. representative compound 42 exhibited potent inhibitory activity,...
Herein we report a highly enantioselective synthesis of polycyclic indoles and pyrroles with up to 99% ee by an iridium catalyst system consisting commercially available precursor readily accessible ligand. Investigation the reaction mechanism led discovery unprecedented dearomatized spiro intermediate its in situ migration phenomenon. The new mode features switching substituent from indole C-3 position C-2 (from case pyrrole) without loss enantiomeric purity, providing novel concept...
Diverse indole-based peri-annulated compounds were synthesized via transition-metal-catalyzed allylic alkylation reaction. With palladium catalyst, nine-membered ring products obtained in 40–70% yields. When iridium catalyst was used, highly enantioenriched seven-membered 40–78% yields and 91–97% ee. Meanwhile, when 3-substituted indole substrates employed with a asymmetric dearomatization of indoles occurred 48–78% 35–78% ee chiral ferrocene-based Phox ligand. Interestingly, an...
Abstract An organic acid catalyzed direct arylation of aromatic C(sp 2 )H bonds in phenols and naphthols for the preparation 1,1′‐linked functionalized biaryls was developed. The products are non‐C ‐symmetrical, atropoisomeric, represent previously untapped chemical space. Overall this transformation is operationally simple, does not require an external oxidant, readily scaled up (up to 98 mmol), structurally diverse 2,2′‐dihydroxy biaryl (i.e., BINOL‐type), as well 2‐amino‐2′‐hydroxy...
We disclosed a novel water-soluble photocatalyst that could promote aerobic oxidative hydroxylation of arylboronic acids to furnish phenols in excellent yields. This transformation uses visible-light irradiation under environmentally friendly conditions, is, catalyst, metal-free, green oxidant, room temperature.
A concise synthesis of spiroindolenines from 2-substituted (Me, Et) indoles and 2-(pyrrolidin-1-yl)benzaldehydes has been developed via a [1,5]-hydride shift/cyclization sequence. This method features wide substrate scope an operationally simple procedure, affording the in good to excellent yields moderate diastereoselectivity (3.5/1 dr). When inseparable mixture spiroindolenine isomers were washed with isopropyl ether after flash chromatography, major could be obtained up >20/1 dr.
Peroxisome proliferator-activator receptors α/δ (PPARα/δ) are regarded as potential therapeutic targets for nonalcoholic steatohepatitis (NASH). However, PPARα/δ dual agonist GFT-505 exhibited poor anti-NASH effects in a phase III clinical trial, probably due to its weak agonistic activity and metabolic stability. Other reported agonists either limited potency or had unbalanced activity. Herein, we report series of novel triazolone derivatives agonists. Among them, compound H11 potent...
An efficient organophosphorus-catalyzed thiocarbonylation reaction of disulfides with carboxylic acids under air conditions was described. Various functional groups on and can be tolerated the present conditions, affording thioesters in good to excellent yields. This method exhibited chemoselectivity applied for late-stage functionalization drug molecules containing a acid group.
Pyruvate production by Torulopsis glabrata was used as a model to study the mechanism of product inhibition and strategy for enhancing pyruvate production. It found that concentration cell growth deceased with increase NaCl sorbitol concentrations. To enhance osmotic stress resistance strain, an NaCl-tolerant mutant RS23 screened selected through pH-controlled continuous culture 70 g/L selective criterion. Compared parent could grow well on medium containing or 0.6 mol/L sorbitol. strain...
An efficient iridium-catalyzed intramolecular Friedel-Crafts-type allylic alkylation reaction of phenols was developed, affording tetrahydroisoquinolines with moderate to excellent yields, enantioselectivity, and good regioselectivity.
Abstract O ‐Aryloximes, generated from readily available and inexpensive oximes through transition‐metal‐free ‐arylation, can either be hydrolyzed to ‐arylhydroxylamines or conveniently converted structurally diverse benzo[ b ]furans an environmentally benign, one‐pot [3,3]‐sigmatropic rearrangement/cyclization sequence.
Abstract An organic acid catalyzed direct arylation of aromatic C(sp 2 )H bonds in phenols and naphthols for the preparation 1,1′‐linked functionalized biaryls was developed. The products are non‐C ‐symmetrical, atropoisomeric, represent previously untapped chemical space. Overall this transformation is operationally simple, does not require an external oxidant, readily scaled up (up to 98 mmol), structurally diverse 2,2′‐dihydroxy biaryl (i.e., BINOL‐type), as well 2‐amino‐2′‐hydroxy...
Expeditious access to oxadiazepines via 1,5-hydride shift/cyclization of pyrrolidine- or tetrahydroisoquinoline-containing nitrones has been developed. With 1,3-dipole serving as the hydride acceptors, this transformation was promoted by a Lewis acid, providing structurally diverse in good yields. A one-pot process for situ nitrone formation, shift, and ring cyclization also realized.
A highly enantioselective synthesis of substituted tetrahydrocarbolines via Ir-catalyzed Friedel–Crafts type intramolecular asymmetric allylic alkylation 2-indolyl allyl carbonates has been developed. This strategy features excellent chemoselectivity and enantioselectivity, mild reaction conditions, an easily accessed chiral ligand.
Bridged indoline derivatives were synthesized by an intermolecular Pd-catalyzed allylic dearomatization reaction of substituted indoles. The between indoles and allyl carbonates bearing a nucleophilic alcohol side-chain proceeds in cascade fashion, providing bridged indolines excellent enantioselectivity.
Abstract We disclose an efficient and operationally simple protocol for the preparation of fused N‐heterocycles starting from readily available 2‐nitrobiaryls PhMgBr under mild conditions. More than two dozen N‐heterocycles, including bioactive natural products, have been synthesized using this method. A stepwise electrophilic aromatic cyclization mechanism was proposed by DFT calculations.
The Rh(<sc>ii</sc>)-catalyzed sulfur ylide [1,2]-rearrangement of carbenoids generated from aryldiazoacetates has been realized <italic>via</italic> N–S bond insertion under low catalyst loading.