A5037760162- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Catalytic Cross-Coupling Reactions
- Catalytic C–H Functionalization Methods
- Synthetic Organic Chemistry Methods
- Melanoma and MAPK Pathways
- Protein Degradation and Inhibitors
- Histone Deacetylase Inhibitors Research
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Computational Drug Discovery Methods
- Synthesis and biological activity
- Chemical Synthesis and Analysis
- Cancer Mechanisms and Therapy
- Synthesis of heterocyclic compounds
- Nanoparticle-Based Drug Delivery
- Multicomponent Synthesis of Heterocycles
- Synthesis and bioactivity of alkaloids
- Synthesis and Biological Evaluation
- Cancer-related Molecular Pathways
- Chronic Lymphocytic Leukemia Research
- Asymmetric Synthesis and Catalysis
- Dendrimers and Hyperbranched Polymers
- Click Chemistry and Applications
- Synthesis and Characterization of Heterocyclic Compounds
- Angiogenesis and VEGF in Cancer
China Pharmaceutical University
2015-2024
A new and stereoselective synthetic approach to spirooxindole 4H-pran-2-one derivatives with three contiguous stereogenic centers has been developed via an NHC-catalyzed three-component domino reaction of alkynyl aldehydes oxindoles. The proceeds smoothly in good yields high diastereoselectivities. These novel heterocyclic spirooxindoles may provide promising candidates for drug discovery. Additionally, a possible mechanism the entire sequence is proposed.
A stereoselective synthetic approach to spirooxindole γ-butyrolactams is developed via N-heterocyclic carbene-catalyzed formal [3 + 2] annulation of α-bromoenals with 3-aminooxindoles. An enantioselective variant this methodology also investigated resulting in good substrate tolerance and high enantioselectivities.
A novel synthesis of spirooxindoles has been developed by cooperative NHC–Lewis acid-mediated formal [3 + 2] annulations alkynyl aldehydes with isatins.
Reported here is a novel photoinduced strategy for the borylation of aryl sulfonium salts using bis(pinacolato)diboron as boron source. This method exploits redox-neutral sulfoniums to gain access radicals via C–S bond activation upon photoexcitation under transition-metal-free conditions. Therefore, it grants diverse arylboronate esters with good performance from easily available accompanied by mild conditions, operational simplicity, and easy scalability.
Photochemical solvent-controlled difluoromethylation and bromo-difluoromethylation reactions of bicyclobutanes are described. The method provides efficient pathways to obtain difluoroalkyl functionalized bioisosteres for drug discovery.
Abstract Enal and ynal‐derived α,β‐unsaturated acylazoliums under N‐heterocyclic carbene (NHC) catalysis have been applied for annulations with indolin‐3‐ones. The two reactions offer a direct efficient access to functionalized 3,4‐dihydropyrano[3,2‐ b ]indol‐2‐ones in moderate high yields, which may provide promising candidates drug discovery.
NIK plays a crucial role in the noncanonical NF-κB signaling pathway associated with diverse inflammatory and autoimmune diseases. Our study presents compound 54, novel inhibitor, designed through structure-based scaffold-hopping approach from previously identified B022. Compound 54 demonstrates remarkable selectivity potency against both vitro vivo, effectively suppressing pro-inflammatory cytokines nitric oxide production. In mouse models, protected LPS-induced systemic sepsis, reducing...
Abstract A novel synthetic method to access fused indolin‐3‐ones with a tetrasubstituted carbon stereocenter has been developed via NHC‐catalyzed umpolung formal [3+3] cycloaddtion of enals isatogens. This methodology could be also applied for the quick construction 6‐5‐5 tricyclic pyrrolo[1,2‐ ]indole skeleton which is frequently found as core structure many indole alkaloids. magnified image
A novel synthetic approach to functionalized indolo[2,3-<italic>a</italic>]quinolizidines is developed <italic>via</italic> an N-heterocyclic carbene-catalyzed annulation of cyclic β-enamino esters with enals.
Spiro and fused indoles are attractive heterocyclic compounds with broad promising activities in various therapeutic fields, thus, have become the synthetic targets of organic chemists. In this account, we describe our recent progress synthesis a series spiro indole derivatives through N-heterocyclic carbene (NHC)-catalyzed annulations diverse NHC-bound intermediates derived from α,β-unsaturated aldehydes. Particularly, novel synthesized isatin-derived α-bromoenals may be used as versatile...
Secondary mutations of FLT3 have become the main mechanism inhibitor resistance that presents a significant clinical challenge. Herein, series pyrazole-3-amine derivatives were synthesized and optimized to overcome common secondary FLT3. The structure-activity relationship molecular dynamics simulation studies illustrated ribose region could be occupied help address obstacle mutations. Among those derivatives, compound 67 exhibited potent selective inhibitory activities against...
β-Functionalization of indolin-2-one-derived aliphatic acids has been applied in formal [3 + 2] annualtions for catalyst-free and divergent synthesis two series structurally interesting 3,3'-spirooxindole γ-butyrolactones that may be attractive potential drug discovery. These findings also pave the way further diversity-oriented spirooxindoles starting from or their derivatives.
A transition-metal-free base catalyzed intramolecular cyclization of 2-ynylphenols was developed for the facile synthesis 2-substituted benzo[b]furans. Various 2-aryl and 2-alkyl substituted benzo[b]furans can be obtained with good to excellent yields using readily available Cs2CO3 as catalyst under mild reaction conditions. The broad substrates scope typical maintenance vigorous efficiency on gram scale make this protocol a potentially practical method synthesize derivatives.
Alkynyl acylammoniums generated in situ from alkynyl acids are first used as electrophilic 3C synthons a formal [3 + 3] annulation with 1,3-dicarbonyl compounds for regioselective synthesis of functionalized 4H-pyran-4-ones via 4-(dimethylamino)pyridine/Lewis acid dual-activation strategy. This protocol paves the way further investigation construction diverse heterocyclic skeletons.
Abstract This work presents a photo‐redox vicinal dichlorination of acrylamides using naturally abundant chlorine source (FeCl 3 ). The LMCT FeCl is responsible for the radical inducement, while tetra‐ n ‐butylammonium decatungstate (TBADT) catalytic system enhanced process. method exhibits extraordinarily mild conditions, not requiring external ligands and low E factors, which enables scalable synthesis.
As an effective target in abnormal angiogenesis-related tumor treatment, VEGFR-2 has small-molecule inhibitors of various scaffolds being approved for treating diseases such as renal carcinoma, non-small cell lung cancer, etc. However, endogenous and acquired drug resistance are still considered to be the main contributors failure clinical candidates. Therefore, development novel is urgently needed market but also challenging. In this work, residues including Asp1046, Ile1025, HIS1026,...