A5063515570- Catalytic C–H Functionalization Methods
- Synthesis and Catalytic Reactions
- Sulfur-Based Synthesis Techniques
- Cyclopropane Reaction Mechanisms
- Chemical Synthesis and Analysis
- Asymmetric Synthesis and Catalysis
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Chemical Synthesis and Reactions
- Nanoparticle-Based Drug Delivery
- Catalytic Cross-Coupling Reactions
- Carbohydrate Chemistry and Synthesis
- Radical Photochemical Reactions
- Asymmetric Hydrogenation and Catalysis
- RNA Interference and Gene Delivery
- Synthesis of Indole Derivatives
- Synthetic Organic Chemistry Methods
- Fluorine in Organic Chemistry
- Natural product bioactivities and synthesis
- Oxidative Organic Chemistry Reactions
- Click Chemistry and Applications
- Synthesis and Biological Evaluation
- Advanced biosensing and bioanalysis techniques
- Drug Transport and Resistance Mechanisms
- Synthesis of β-Lactam Compounds
Sichuan University
2016-2025
Buchang Pharma (China)
2025
Fujian Medical University
2025
Union Hospital
2025
Dalian Medical University
2024
Beijing Union University
2021-2022
Zhejiang Yuexiu University
2022
Chongqing Medical University
2021
State Key Laboratory of Biotherapy
2007-2021
Chengdu University
2014-2020
Michael–Michael–retro-Michael cascade reactions are promoted by the highly efficient organocatalyst 9-amino-9-deoxyepiquinine (1). The asymmetric direct vinylogous Michael addition of α,α-dicyanoalkenes to α,β-unsaturated ketones may be followed an intramolecular and a retro-Michael reaction afford polysubstituted 2-cyclohexen-1-one derivatives with high enantioselectivity (see example).
Hydrogen bonding makes a difference: Multifunctional primary amine catalysts derived from cinchona alkaloids are used in the highly enantioselective 1,3-dipolar cycloaddition of cyclic enones and azomethine imines (see scheme; R=aryl, alkyl; TIPBA=2,4,6-triisopropylbenzenesulfonic acid). The synergistic hydrogen-bonding interaction catalyst 1,3-dipole is essential for stereocontrol. Supporting information this article available on WWW under...
The first direct asymmetric vinylogous Mannich (AVM) reaction of α,α-dicyanoolefins and N-Boc aldimines was described promoted by a simple chiral bifunctional thiourea-tertairy amine organocatalyst. highly efficient (S/C up to 1000) regio-, stereoselective (generally >99% de, 96 >99.5% ee) at room temperature for broad array substrates. Enantiomerically pure δ-amino acid could be smoothly prepared from the adduct.
The C3-selective enantioselective Michael-type Friedel–Crafts alkylations of indoles with nonchelating α,β-unsaturated alkyl ketones, catalysed by a chiral primary amine derived from natural cinchonine, were investigated. reactions, in the presence 30 mol% catalyst, smoothly conducted at 0 to −20 °C. Moderate good ee (47–89%) has been achieved.
Background: An intimidating challenge to transporting drugs into the brain parenchyma is presence of blood–brain barrier (BBB). Glucose an essential nutritional substance for function sustenance, which cannot be synthesized by brain. Its transport primarily depends on glucose transporters capillary endothelial cells. In this paper, brain-targeted properties glucose-modified liposomes using polyethylene glycols with different chain lengths as linkers were compared and evaluated establish...
Selective synthesis of indoles and quinazolines was achieved through a precise control C–H activation/annulation by changing additives.
Abstract Bipyrazolidin‐3‐one derivatives are biologically significant compounds and their importance has increased in the past decades. In this paper, first stereoselective [3 + 2] dipolar cycloadditions of azomethine imines with α,β‐unsaturated aldehydes catalyzed by readily available α,α‐diarylprolinol salts reported, providing a facile route to synthesis various chiral bipyrazolidin‐3‐one under mild conditions. The organocatalyst 1 g strongly electron‐withdrawing groups exhibited best...
The bifunctional thiourea–tertiary amine derivatives of simple chiral diamines serve as highly enantioselective catalysts for the Michael addition α-substituted cyanoacetates to vinyl sulfones, giving an efficient protocol construction all-carbon substituted quaternary stereocentre.
The asymmetric Michael-type Friedel–Crafts reaction of naphthols and nitroolefins promoted by bifunctional thiourea–tertiary amine organocatalysts (up to 95% ee) was investigated; on simply extending the time further cascade reactions could occur generate enantiopure dimeric tricyclic 1,2-dihydronaphtho[2,1-b]furanyl-2-hydroxylamine derivatives.
The first highly regio-, chemo-, diastereo- and enantioselective direct vinylogous Michael addition of α,α-dicyanoolefins to α,β-unsaturated aldehydes is described, employing readily available chiral α,α-diarylprolinol salts as iminium organocatalysts.
Michael-Michael-retro-Michael-Kaskadenreaktionen gelingen mithilfe des hocheffizienten Organokatalysators 9-Amino-9-desoxyepichinin (1). Der asymmetrischen direkten vinylogen Michael-Addition von α,α-Dicyanalkenen an α,β-ungesättigte Ketone können sich eine intramolekulare und Retro-Michael-Reaktion anschließen, wobei mehrfach substituierte 2-Cyclohexen-1-on-Derivate mit hoher Enantioselektivität entstehen (siehe Beispiel).
New glycosyl derivative of cholesterol was synthesized as a material for preparing novel liposome to overcome the ineffective delivery normal drug formulations brain by targeting (glucose transporters) GLUTs on BBB. Coumarin-6 used fluorescent probe. The results have shown that cytotoxicity capillary endothelial cells (BCECs) glucose-mediated containing coumarin-6 less than conventional liposome. BBB model in vitro established coculturing BCECs and astrocytes (ACs) rat test transendothelial...
An iridium-catalyzed B–H bond insertion reaction between borane adducts and sulfoxonium ylides to afford α-boryl carbonyls has been developed. The starting materials are safe readily available. In addition, analogues of ylides, such as sulfonium salts could also be amenable the reaction.
A water-mediated C–H activation using sulfoxonium ylides is reported, providing a general, green and step-economic approach to construct C–C bond varieties of useful N-heterocycle scaffolds.
A mild and facile photo-induced cascade radical addition/cyclization of unactivated alkenes has been reported, through which a variety biologically valuable phosphine-containing quinazolinones could be obtained in moderate to good yields. The protocol was characterized by conditions, broad substrate scope, high atomic economy.
Neurodegenerative diseases (NDDs) are mainly induced by oxidative stress which produces excessive reactive oxygen species (ROS). Quercetin (QU) is a potent antioxidant with some effects on NDDs. This study prepared and characterized novel glucose-modified QU liposome (QU–Glu–Lip), aiming not only to overcome QU’s poor water solubility bioavailability but also deliver more brain tissue enhance its neuroprotective effect. QU–Glu–Lip possessed encapsulation efficiency (EE) of 89.9%, homogenous...
The chemoselective ring opening of N-tosyl aziridines with aldehydes catalyzed by an N-heterocyclic carbene was investigated under aerobic conditions. Unexpected carboxylates 1,2-amino alcohols from the corresponding aldehydes, rather than acyl anion ring-opened β-amino ketones, were exclusively obtained. A plausible mechanism for this unprecedented carbene-mediated reaction also proposed.
Die H-Brücke macht den Unterschied: Primäre Amine mit Cinchona-Alkaloid-Gerüst katalysieren die hoch enantioselektive 1,3-dipolare Cycloaddition von cyclischen Enonen und Azomethiniminen (siehe Schema; R=Aryl, Alkyl; TIPBA=2,4,6-Triisopropylbenzolsulfonsäure). synergistische Wasserstoffbrücke zwischen dem Katalysator 1,3-Dipol steuert stereochemischen Verlauf der Reaktion.
A recurrent neural network(RNN) based dynamic back propagation(BP) algorithm model with historical internal inputs are developed to predict the temperature and humidity of a solar greenhouse in north China. Climate data including air substrate temperature, humidity, illumination C02 concentration recorded over eight days were used build validate models for climatic prediction. In order compare accuracy predictions, different performance measures, such as average relative error (ARE), mean...