879507-06-9

Upstream product

• 33397-21-6 tris(4-methoxyphenyl)bismuth 
• 120681-06-3 (E)-3-(2-chlorophenyl)acryloyl chloride 
• 704-96-1 trans-2-chlorocinnamic acid 
• 100-66-3 methoxybenzene 
• 20912-79-2 4-methoxyphenacylidene dimethylsulphurane 
• 107135-19-3 N’-(2-chlorobenzylidene)-4-methylbenzenesulfonohydrazide 
• 89-98-5 2-chloro-benzaldehyde 
• 100-06-1 1-(4-methoxyphenyl)ethanone 

Downstream Products

• 489398-73-4 5-(2-chlorophenyl)-3-(4-methoxyphenyl)-1-phenyl-4,5-dihydro-1H-pyrazole 
• 1380820-14-3 C₂₂H₁₉ClN₂O 

Relevant academic research and scientific papers

Alkene Synthesis by Photo-Wolff-Kischner Reaction of Sulfur Ylides and N-Tosylhydrazones

A visible-light-driven and room temperature photo-Wolff-Kischner reaction of sulfur ylides and N-tosylhydrazones has been developed for the first time to provide modular access to alkene synthesis. The high functional group tolerance and broad substrate scope were demonstrated by more than 60 examples. Both E- and Z-olefinic stereochemistry in the products could be controlled with excellent stereoselectivity. A series of mechanistic studies support that the reaction should proceed through a radical-carbanion crossover pathway, specifically involving addition of photo-generated sulfur ylide radical cations to N-tosylhydrazones to form carbanions and subsequent Wolff-Kischner process.

Method using Ti (III) complex catalytic alkyne selective hydrogenation reduction to prepare chalcone compounds

The invention discloses a method for preparing chalcone compounds through selective hydrogenation of Ti (III) complexes to prepare chalcone compounds, wherein zinc powder is used as a catalyst, zinc powder is a reducing agent, triethylamine hydrochloride is a proton source, and an alkyne and triethylamine hydrochloride are subjected to radical selective addition reaction under the protection of inert gas to generate chalcone compounds. The reaction condition is mild, the operation is simple, the reaction time is short, the reaction product is single, the atom economy is high, and only the product needs to be separated by simple column chromatography after the reaction is finished. The chalcone compound has wide biological activity and medicinal value.

Design and synthesis of novel 1,3,5-triphenyl pyrazolines as potential anti-inflammatory agents through allosteric inhibition of protein kinase Czeta (PKCζ)

Much light has been shed on the vital role of protein kinase Czeta (PKCζ) in NF-κB activation and the potential use of PKCζ inhibitors as anti-inflammatory agents. We previously reported a series of 1,3,5-trisubstituted pyrazolines as potent and selective

CBr4 as a Halogen Bond Donor Catalyst for the Selective Activation of Benzaldehydes to Synthesize α,β-Unsaturated Ketones

CBr4 has been employed as a halogen bond donor catalyst for the selective activation of aldehyde, to achieve an efficient solvent- and metal-free CC bond forming reaction in the presence of strong acid sensitive groups such as methoxy, cyanide, ester, and ketal for the synthesis of α,β-unsaturated ketones. This unique capability of CBr4 to act as a halogen bond donor has been explored and established using UV-vis as well as IR spectroscopy. Moreover, this unprecedented methodology enables the synthesis of the pharmaceutically important molecule licochalcone A.

Chalcone derivative and application thereof in regulation of 11beta-HSD1 and prevention and treatment of metabolic syndrome

The invention relates to a chalcone derivative, the structural formula of which is as shown in a formula I, wherein Y is selected from halogen, C1-C6 alkoxyl, hydroxyl and carboxyl; Z is selected from C1-C6 alkoxyl and NR1R2; and R1 and R2 are independently selected from H and C1-C6 alkyl. The chalcone derivative provided by the invention can increase the activity of 11beta-HSD1 oxidase while reducing the activity of the 11beta-HSD1 oxidase, so that the cortisol level of glucocorticoid can be obviously reduced, and the blood glucose level and the blood level are obviously reduced. Therefore, the chalcone derivative is quite effective to treat or prevent metabolic diseases and type 2 diabetes. The formula is as shown in the description.

Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors

We have synthesized three categories of α,β-unsaturated carbonyl derivatives and evaluated their MAO-A and MAO-B inhibitory activities. Among them, compound 10b including α,β-unsaturated ketone group showed the most potent and selective MAO-B inhibitory activity (IC50 human MAO-B 16 nM, >6000-fold selective vs MAO-A) and compound 10b exhibited good reversibility compared with selegiline, a well-known irreversible MAO-B inhibitor. However, both α,β-unsaturated amide and ester derivatives exhibited weaker MAO-B inhibition potencies. The docking studies provided insights into the possible binding modes and the key interaction sites of the synthesized MAO-B inhibitors.

Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53

Derivatives with scaffolds of 1,3,5-tri-substituted pyrazoline and 1,3,4,5-tetra-substituted pyrazoline were synthesized and tested for their inhibitory effects versus the p53+/+ HCT116 and p53-/- H1299 human tumor cell lines. Severa

A new and direct synthesis of chalcones via TFAA-H3PO 4 mediated c-c bond forming reaction

A number of α,β-unsaturated carboxylic acids were reacted with electron rich arenes or heteroarene in the presence of trifluoroacetic anhydride (TFAA) and H3PO4 at room temperature to give a variety of chalcone derivatives in good to

Evaluation and discovery of novel synthetic chalcone derivatives as anti-inflammatory agents

Major anti-inflammatory agents, steroids and cyclooxygenase, were proved to have serious side effects. Here, a series of chalcone derivatives were synthesized and screened for anti-inflammatory activities. QSAR study revealed that the presence of electron-withdrawing groups in B-ring and electron-donating groups in A-ring of chalcones was important for inhibition of LPS-induced IL-6 expression. Further, compounds 22, 23, 26, 40, and 47 inhibited TNF-α and IL-6 release in a dose-dependent manner and decreased LPS-induced TNF-α, IL-1β, IL-6, IL-12, and COX-2 mRNA production. Mechanistically, compounds 23 and 26 interfered with JNK/NF-κB signaling and dose-dependently prevented ERK and p38 activation. In addition, 23 and 26 exhibited a significant protection against LPS-induced death and were able to block high glucose-activated cytokine profiles in macrophages. Together, these data show a series of anti-inflammatory chalcones with potential therapeutic effects in inflammatory diseases.

Screening of biological activities of a series of chalcone derivatives against human pathogenic microorganisms

In an effort to develop new antimicrobial agents, a series of chalcone derivatives, 3-60, were prepared by Claisen-Schmidt condensation of appropriate acetophenones and 2-furyl methyl ketones with appropriate aromatic aldehydes, furfural, and thiophene-2-carbaldehyde in an aqueous solution of NaOH and EtOH at room temperature. The synthesized compounds were characterized by means of their IR- and NMR-spectral data, and elemental analysis. All compounds were tested for their antibacterial and antifungal activities by the disc diffusion method. For the most active compounds, also minimum inhibitory concentrations (MICs) were determined.