75175-76-7

Upstream product

• 445-27-2 2'-Fluoroacetophenone 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 

Downstream Products

• 1257317-83-1 C₁₂H₇FN₂S 
• 877129-18-5 2-(3-N,N-dimethylamino-prop-2-en-1-onyl)phenyldiphenylphosphine 
• 1350639-41-6 C₆H₄P(C₆H₅)2C₄N₂H₂N(CH₃)2 
• 1350639-37-0 C₆H₄P(C₆H₅)2C₄N₂H₂NH₂ 
• 1350639-40-5 C₆H₄P(C₆H₅)2C₄N₂H₂NHC₂H₅ 
• 1350639-42-7 C₆H₄P(C₆H₅)2C₄N₂H₂N(CH₂)4 
• 1350639-43-8 C₆H₄P(C₆H₅)2C₄N₂H₂N(CH₂)5 
• 1354628-20-8 6-(2-fluorophenyl)-1,2-dihydro-2-phenylpyrazolo[3,4-b]pyridin-3-one 
• 1354628-23-1 6-(2-fluorophenyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine 

Relevant academic research and scientific papers

Access to α,α-dihaloacetophenones through anodic C[dbnd]C bond cleavage in enaminones

We have developed a method to synthesize α,α-dihaloketones under electrochemical conditions. In this reaction, the Cl- or Br- is oxidized to Cl2 or Br2 at the anode, which undergoes two-step addition reactions with the N,N-dimethyl enaminone, and finally breaks C[dbnd]C of the N,N-dimethyl enaminone to generate α,α-dihaloketones. The electrosynthesis reaction can be conveniently carried out in an undivided electrolytic cell at room temperature. In addition, various functional groups are compatible with this green protocol which can be applied simultaneously to the gram scale without significantly lower yield.

I2-Promoted [4 + 2] cycloaddition of: In situ generated azoalkenes with enaminones: Facile and efficient synthesis of 1,4-dihydropyridazines and pyridazines

A facile and efficient strategy for the synthesis of 1,4-dihydropyridazines and pyridazines through I2-promoted [4 + 2] cycloaddition of in situ generated azoalkenes with enaminones has been developed. The switch in selectivity is attributed to the judici

1-phenyl-3-benzenemethylamido-2-propylene-1-ketone compounds and preparation method and use thereof

The invention provides 1-phenyl-3-benzenemethylamido-2-propylene-1-ketone compounds and a preparation method and use thereof. The compounds are a series of compounds with brand-new structures, have a very good inhibitory effect on aggregation of A beta protein, meanwhile, can also be used for inhibiting the aggregation of Tau proteins and can be used for developing drugs for treating neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease.

Bimetallic Cu/Pd Catalysts with Bridging Aminopyrimidinyl Phosphines for Decarboxylative Cross-Coupling Reactions at Moderate Temperature

A bimetallic catalyst system is presented that enables the decarboxylative cross-coupling of triflates with carboxylate salts at only 100 °C, which is 70 °C lower than with previous Cu/Pd-based systems. The new protocol allows the coupling of a broad range of aryl triflates with various substituted 2-nitrobenzoates in good to excellent yields. The key feature of the catalyst system is a bidentate P,N-ligand designed to bridge the Pd and Cu centres and thereby facilitating the rate-determining transmetalation step. Mass spectrometry (ESI-MS) studies support the ability of the aminopyrimidinyl phosphine to simultaneously coordinate copper and palladium.

Discovery and structure-activity relationships study of novel thieno[2,3-b]pyridine analogues as hepatitis C virus inhibitors

Current treatment for hepatitis C is barely satisfactory, there is an urgent need to develop novel agents for combating hepatitis C virus infection. This study discovered a new class of thieno[2,3-b]pyridine derivatives as HCV inhibitors. First, a hit compound characterized by a thienopyridine core was identified in a cell-based screening of our privileged small molecule library. And then, structure activity relationship study of the hit compound led to the discovery of several potent compounds without obvious cytotoxicity in vitro (12c, EC50 = 3.3 μM, SI >30.3, 12b, EC50 = 3.5 μM, SI >28.6, 10l, EC50 = 3.9 μM, SI >25.6, 12o, EC 50 = 4.5 μM, SI >22.2, respectively). Although the mechanism of them had not been clearly elucidated, our preliminary optimization of this class of compounds had provided us a start point to develop new anti-HCV agents.

Novel thienopyridine derivatives as specific anti-hepatocellular carcinoma (HCC) agents: Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation

Novel thienopyridine derivatives 1b-1r were synthesized, based on a hit compound 1a that was found in a previous cell-based screening of anticancer drugs. Compounds 1a-1r have the following features: (1) their anticancer activity in vitro was first reported by our group. (2) The most potent analog 1g possesses hepatocellular carcinoma (HCC)-specific anticancer activity. It can specifically inhibit the proliferation of the human hepatoma HepG2 cells with an IC50 value of 0.016 μM (compared with doxorubicin as a positive control, whose IC50 was 0.37 μM). It is inactive toward a panel of five different types of human cancer cell lines. (3) Compound 1g remarkably induces G0/G1 arrest and apoptosis in HepG2 cells in vitro at low micromolar concentrations. These results, especially the HCC-specific anticancer activity of 1g, suggest their potential in targeted chemotherapy for HCC.