75415-00-8

Upstream product

• 1122-62-9 2-acetylpyridine 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 1188-33-6 N,N-dimethylformamide diethyl diacetal 
• 127-19-5 N,N-dimethyl acetamide 
• 98-86-2 acetophenone 
• 25408-61-1 Ν,Ν-dimethylacetamide dimethyl acetal 
• 68-12-2 N,N-dimethyl-formamide 

Downstream Products

• 75415-03-1 2-(1H-pyrazol-3-yl)pyridine 
• 138785-70-3 (+)-2-<1-(1-Phenylethyl)-5-pyrazolyl>pyridin 
• 1148-79-4 2,2':6,2''-terpyridine 
• 938066-21-8 2-(1-methyl-1H-5-pyrazolyl)pyridine 
• 162435-06-5 1-methyl-3-(pyridin-2-yl)-1H-pyrazole 
• 35299-71-9 2,6-bis(thiophen-2-yl)pyridine 
• 123760-40-7 6-(thiophen-2-yl)-2,2'-bipyridine 
• 320416-38-4 7-(2-pyridyl)-1,2,4-triazolo[1,5-a]pyrimidine 
• 66521-65-1 4-(pyridin-2-yl)pyrimidine-2-ylamine 
• 872672-74-7 N-(4-methyl-3-(4-(pyridin-2-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl) benzamide 
• 881677-39-0 4-chloromethyl-N-[4-methyl-3-(4-pyridin-2-yl-pyrimidin-2-ylamino)-phenyl]-benzamide 
• 475587-24-7 N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyridinamine 
• 475587-23-6 N-(2-methyl-5-nitrophenyl)-4-(pyridin-2-yl)pyrimidin-2-amine 
• 676479-88-2 methyl 2-(3-(pyridin-2-yl)-1H-pyrazol-1-yl)acetate 

Relevant academic research and scientific papers

Stereoselective synthesis of trifluoromethyl-substituted 2: H -furan-amines from enaminones

A straightforward strategy for synthesis of highly functionalized trifluoromethyl 2H-furans is described. The copper catalyzed method relies on a cascade cyclic reaction between enaminones and N-tosylhydrazones. This method allows the synthesis of 2-amino

Method for large-scale production α, α, α .

The invention discloses a method for large-scale production α, α, α . The reaction operation in Step a was as follows: At room temperature 2 - acetyl pyridine was added. Then N mL of N -dimethyl formamide dimethyl acetal and a catalyst are added to the organic solvent, and after the reaction is completed, the reaction solution is poured into an aqueous sodium hydroxide solution, and then the resulting organic phase is washed, dried, concentrated and recrystallized to obtain an intermediate: 1 - (3 - pyridyl) -3 - (dimethylamino) -2 - propylene -1 - ketone. The method disclosed by the invention is easy to implement large-scale production, high in yield, low in cost, simple to operate and mild in reaction condition.

Structure-dependent regioselectivity of a roll-over cyclopalladation occuring at 2,2′-bipyridine-type ligands

In this work, different bipyridine-analogue ligands bearing a dimethylamino group in the meta-position of one of the heterocyclic rings were synthesized and reacted with palladium(II) acetate under identical conditions. Cyclometallated palladium(II) complexes with C,N- or C,N,N’-coordinating chelate ligands are formed which were characterized by elemental analysis, 1H and 13C NMR spectroscopy, and single crystal X-ray diffraction analysis. In the case of the mononuclear, C,N,N’-coordinated complex, which is formed by an attack of the palladium(II) site at of the N-methyl groups, the primarily coordinating acetato ligand is exchanged against a chlorido ligand, which is liberated from the solvent dichloromethane by a nucleophilic substitution reaction. In contrast, cyclometallation occurring at one of the six-membered heterocycles leads to dinuclear acetato-bridged palladium(II) complexes.

A family of polyoxometalate-resorcin[4]arene-based metal–organic materials: Assemblies, structures and lithium ion battery properties

Polyoxometalates (POMs) are alternative anode materials of lithium ion batteries (LIBs) for their reversible electrochemical redox behaviors and electron storage functions. To overcome the low conductivity and poor stability of the POMs, embedment of POMs into metal–organic hybrid complexes is a promising synthetic strategy. Here, we designed a family of copper-containing POM-resorcin[4]arene-based complexes supported by a resorcin[4]arene ligand (TPTR4A), copper cations and Keggin-type POMs, namely, [Cu4(TPTR4A)2][PMo12O40](OH)·2DMA·H2O (1a), [Cu4(TPTR4A)2][SiW12O40]·2.5DMA (1b) and [Cu4(TPTR4A)2][PW12O40](OH)·0.5DMA·5H2O (1c) (DMA = N,N’-dimethylacetamide). To improve the conductivity of the complexes, composites 1a@GO-1c@GO were obtained through mechanical grinding of the complexes and graphene oxide (GO). Strikingly, they show high initial specific capacity and stability for LIBs. This work offered a strategy for application of the POM-based complexes as LIBs via combining POM-based complexes and RGO.

Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- And BCRP-Mediated Multidrug Resistance

Overexpression of ATP binding cassette (ABC) transporters, including P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), is an important factor leading to multidrug resistance (MDR) in cancer treatments. Three subclasses of dual inhibitors of P-gp and BCRP were designed based on the active moieties of BCRP inhibitors, tyrosine kinase inhibitors, and P-gp inhibitors, of which compound 21 possessed low cytotoxicity, high reversal potency, and good lipid distribution coefficient. 21 also increased the accumulation of Adriamycin (ADM) and Mitoxantrone (MX), blocked Rh123 efflux, and made no change in the protein expression of P-gp and BCRP. Importantly, coadministration of 21 can significantly improve the oral bioavailability of paclitaxel (PTX). It was also demonstrated that 21 significantly inhibited the growth of K562/A02 xenograft tumors by increasing the sensitivity of ADM in vivo. In summary, 21 has the potential to overcome MDR caused by P-gp and BCRP and to improve the oral bioavailability of PTX.

Synthesis method of 3-formyl indole derivatives

The invention discloses a synthesis method of 3-formyl indole derivatives. The method comprises the following steps: reacting 3-(dimethylamino)-1-(2-pyridyl)-2-propenone with N-substituted aniline ina solvent under the actions of a palladium catalyst and an oxidant, and carrying out after-treatment after the reaction finishes to obtain the 3-formyl indole derivatives. According to the method, a C-H/C-H cross dehydrogenation coupling strategy serves as a key step, seven 3-formyl indole derivatives with potential activity are simply and conveniently synthesized, and raw materials used in the method are cheap, simple and easy to obtain.

Synthesis and biological evaluation of (3/4-(pyrimidin-2-ylamino)benzoyl)-based hydrazine-1-carboxamide/carbothioamide derivatives as novel RXRα antagonists

Abnormal alterations in the expression and biological function of retinoid X receptor alpha (RXRα) have a key role in the development of cancer. Potential modulators of RXRα as anticancer agents are explored in growing numbers of studies. A series of (4/3-(pyrimidin-2-ylamino)benzoyl)hydrazine-1-carboxamide/carbothioamide derivatives are synthesised and evaluated for anticancer activity as RXRα antagonists in this study. Among all synthesised compounds, 6A shows strong antagonist activity (half maximal effective concentration (EC50) = 1.68 ± 0.22 μM), potent anti-proliferative activity against human cancer cell lines HepG2 and A549 cells (50% inhibition of cell viability (IC50) values 50 values > 100 μM). Further bioassays indicate that 6A inhibits 9-cis-RA-induced activity in a dose-dependent manner, and selectively binds to RXRα-=LΒD with submicromolar affinity (Kd = 1.20 × 10?7 M). 6A induces time-and dose-dependent cleavage of poly ADP-ribose polymerase, and significantly stimulates caspase-3 activity, leading to RXRα-dependent apoptosis. Finally, molecular docking studies predict the binding modes for RXRα-LBD and 6A.

COMPOUNDS AND METHODS FOR HEMATOPOIETIC REGENERATION

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

Whole microwave syntheses of pyridylpyrazole and of Re and Ru luminescent pyridylpyrazole complexes

The synthesis of 3-(2pyridyl)pyrazole (pypzH) by conventional methods requires refluxing at high temperatures during more than 16 h, but this is reduced to two consecutive steps of 2 h at 100 °C, and of 10 min at 50 °C in a microwave (MW) assisted synthesis. Its coordination as chelating ligand to the “fac-ReIBr(CO)3” and “RuII(bipy)2” fragments also occurs MW assisted in 5 or 10 min, respectively. A new MW assisted synthetic method is also described for the synthesis of the starting material [Ru(bipy)2Cl2]·2H2O. Both pypzH complexes are characterized by X-ray crystallography, and the study of their photophysical properties support their phosphorescence. The electrochemistry of the Ru complex indicates that electrochemical oxidation is followed by a chemical process.

Excited-State Kinetics of an Air-Stable Cyclometalated Iron(II) Complex

The complex class [Fe(N^N^C)(N^N^N)]+ with an Earth-abundant metal ion has been repeatedly suggested as a chromophore and potential photosensitizer on the basis of quantum chemical calculations. Synthesis and photophysical properties of the parent complex [Fe(pbpy)(tpy)]+ (Hpbpy=6-phenyl-2,2′-bipyridine and tpy=2,2′:6′,2′′-terpyridine) of this new chromophore class are now reported. Ground-state characterization by X-ray diffraction, electrochemistry, spectroelectrochemistry, UV/Vis, and X-ray spectroscopy in combination with DFT calculations proves the high impact of the cyclometalating ligand on the electronic structure. The photophysical properties are significantly improved compared to the prototypical [Fe(tpy)2]2+ complex. In particular, the metal-to-ligand absorption extends into the near-IR and the 3MLCT lifetime increases by 5.5, whereas the metal-centered excited triplet state is very short-lived.