Category: 3731-53-1

Wang, Chao; Rui, Xiyan; Si, Dongjuan; Dai, Rupeng; Zhu, Yueyue; Wen, Hongmei; Li, Wei; Liu, Jian published the artcile< Copper-Catalyzed Three-Component Cascade Reaction of Benzaldehyde with Benzylamine and Hydroxylamine or Aniline: Synthesis of 1,2,4-Oxadiazoles and Quinazolines>, Quality Control of 3731-53-1, the main research area is aryl aldehyde aromatic amine copper catalyst tandem cyclization; biaryl oxadiazole preparation green chem; benzaldehyde benzylamine copper catalyst tandem cyclization green chem; diphenyl quinazoline preparation.

The analogous three-component synthesis strategy for substituted 1,2,4-oxadiazoles and quinazolines derivatives from readily available benzaldehydes, benzylamines and hydroxylamine or anilines was developed. Both the cascade reaction sequences involved nucleophilic addition of C-N bond, introduction a halogen donor, nucleophilic substitution and Cu(II)-catalyzed aerobic oxidation This synthesis methodol. demonstrated good yields, broad substrate scope and oxygen as a green oxidant. Thus, this synthesis protocol provided strategies for the construction of substituted 1,2,4-oxadiazole and quinazolines from readily and simple starting materials.

Advanced Synthesis & Catalysis published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Quality Control of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Jinguo; Yin, Feng; Hu, Jun; Ju, Yong published the artcile< Cu2+-triggered shrinkage of a natural betulin-derived supramolecular gel to fabricate moldable self-supporting gel>, Category: pyridine-derivatives, the main research area is copper ion shrinkage betulin supramol gel moldable self supporting.

Most supramol. gels have a poor ability to be molded into well-defined shapes, preventing them from having the same potential as clay-based and polymeric gels in applications. In this research, a natural betulin-derived bola-type amphiphile Py-BL was synthesized and found to assemble into a supramol. gel with left-handed helixes driven by hydrogen bonding and hydrophobic interactions. Due to the pyridine groups, which were able to coordinate metal ions and were sensitive to acidity, the resulting Py-BL gel exhibited responses to certain metal ions, and Cu2+-selective gel shrinkage was observed, with a contraction of the gel phase in three dimensions. The coordination between Cu2+ and pyridine groups in the ratio of 1 : 4 led to a cross-linked network of nanofibers and decreased the hydrophilic performance of the Py-BL gel, consequently causing the gelling solvent to extrude from the gel network with a macroscopic gel shrinkage. This Cu2+-triggered shrunken gel exhibited an improved rheol. strength and could self-demold spontaneously through the shrinkage process with a precise amount of Cu2+. Using this strategy, we fabricated moldable self-supporting supramol. gels with designed shapes and elec. conductivity It is believed that the Cu2+-triggered shrinkage provides a novel approach to the fabrication of moldable self-supporting supramol. gels at ultralow gel loadings.

Materials Chemistry Frontiers published new progress about Fluorescence. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Beebeejaun-Boodoo, B. M. P.; Rademeyer, Melanie published the artcile< Coordination polymers and metallocycles of metal halides with n-(aminomethyl)pyridine, n = 3 or 4: Structures and solid-state fluorescence>, Name: Pyridin-4-ylmethanamine, the main research area is cobalt mercury halo aminomethylpyridine coordination polymer metallocycle preparation; crystal structure cobalt mercury halo aminomethylpyridine coordination polymer metallocycle; fluorescence cobalt mercury halo aminomethylpyridine coordination polymer metallocycle.

Coordination polymers and metallocycles formed by the reactions of CoX2 or HgX2, X = Cl-, Br- or I-, with the ditopic organic ligands (L) 3-(aminomethyl)pyridine, 3amp, or 4-(aminomethyl)pyridine, 4amp, are reported. The combination of L = 4amp with CoCl2, CoBr2 or HgI2 yielded one-dimensional coordination polymers of composition [M(L)(X)2]∞, in which the metal ion displays a tetrahedral geometry. Only the combination of L = 3amp with CoCl2 gave a one-dimensional coordination polymer, while the rest of the structures containing this organic ligand were comprised of metallocycles. The metallocyclic rings have a composition [M2(L)2(X)4]n, with n = 1 for L = 3amp and HgBr2, and n = 2 for L = 3amp and CoBr2 or HgI2. Strong N-H. X-M hydrogen bonding interactions are observed in both the coordination polymer and metallocycle structures. The solid-state fluorescence spectra of selected compounds are reported.

Polyhedron published new progress about Coordination polymers Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Name: Pyridin-4-ylmethanamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Shuni; Yang, Hong; Su, Mingbo; Lian, Fulin; Cong, Zhanqing; Wei, Rongrui; Zhou, Yubo; Li, Xingjun; Zheng, Xingling; Li, Chunpu; Fu, Xuhong; Han, Xu; Shi, Qiongyu; Li, Cong; Zhang, Naixia; Geng, Meiyu; Liu, Hong; Li, Jia; Huang, Xun; Wang, Jiang published the artcile< 5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma>, Formula: C6H8N2, the main research area is aminonaphthalene sulfonamide preparation NSD2 inhibitor SAR antitumor apoptosis human; 5-Aminonaphthalene derivatives; HTS; Inhibitor; Methyltransferase; Multiple myeloma; NSD2.

Using high-throughput screening (HTS) with biol. analyzes, a series of 5-aminonaphthalene derivatives such as I [X = CO, SO2; R1 = NHCH2Ph, NHPh, NHCH2(4-FC6H4), etc.; R2 = H, NH2, NMe2, etc.] were designed and synthesized as novel NSD2 inhibitors. Among all the prepared compounds, I [R1 = NHCH2Ph, R2 = NH2] displayed a good NSD2 inhibitory activity (IC50 = 2.7μM) and selectivity against both SET-domain-containing and non-SET-domain-containing methyltransferases. Preliminary research indicated the inhibition mechanism of compound I [X = SO2, R1 = NHCH2Ph, R2 = NH2 (II)] by significantly suppressed the methylation of H3K36me2. Compound II specifically inhibited the proliferation of the human B cell precursor leukemia cell line RS4:11 and the human myeloma cell line KMS11 by inducing cell cycle arrest and apoptosis with little cytotoxicity. It was reported that the anti-cancer effect of compound II was partly achieved by completely suppressing the transcriptional activation of NSD2-targeted genes.

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Formula: C6H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zheng, Qiang; Kurpiewska, Katarzyna; Domling, Alexander published the artcile< SNAr Isocyanide Diversification>, COA of Formula: C6H8N2, the main research area is imino isocyanide preparation; isocyanide amine multicomponent nucleophilic aromatic substitution.

The first-time isocyanide diversification based on nucleophilic aromatic substitution of suitable precursor isocyanides like 1-fluoro-4-isocyano-2-nitrobenzene has been described. The mild conditions allow for easy access to multiple novel isocyanides I (R = morpholin-4-yl, pyrrolidin-1-yl, piperidin-1-yl, etc.) useful in organic synthesis. The resulting isocyanides I are solid and non-noxious, yet react nicely in multicomponent reactions.

European Journal of Organic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, COA of Formula: C6H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Domarco, Olaya; Kieler, Claudia; Pirker, Christine; Dinhof, Carina; Englinger, Bernhard; Reisecker, Johannes M.; Timelthaler, Gerald; Garcia, Marcos D.; Peinador, Carlos; Keppler, Bernhard K.; Berger, Walter; Terenzi, Alessio published the artcile< Subcellular Duplex DNA and G-Quadruplex Interaction Profiling of a Hexagonal PtII Metallacycle>, HPLC of Formula: 3731-53-1, the main research area is platinum metallacycle duplex DNA quadruplex interaction; G-quadruplex; SCC; metallacycle; platinum; subcellular localization.

Metal-driven self-assembly afforded a multitude of fascinating supramol. coordination complexes (SCCs) with applications as catalysts, host-guest, and stimuli-responsive systems. However, the interest in the biol. applications of SCCs is only starting to emerge and thorough characterization of their behavior in biol. milieus is still lacking. Herein, we report on the synthesis and detailed in-cell tracking of a Pt2L2 metallacycle. We show that our hexagonal supramol. accumulates in cancer cell nuclei, exerting a distinctive blue fluorescence staining of chromatin resistant to UV photobleaching selectively in nucleolar G4-rich regions. SCC co-localizes with epitopes of the quadruplex-specific antibody BG4 and replaces other well-known G4 stabilizers. Moreover, the photophys. changes accompanying the metallacycle binding to G4s in solution (fluorescence quenching, absorption enhancement) also take place intracellularly, allowing its subcellular interaction tracking.

Angewandte Chemie, International Edition published new progress about Biocompatibility. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, HPLC of Formula: 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shi, Wei; Zhang, Ping; Zou, Feng; Zhou, Jiaqi; Yin, Ziyu; Cai, Zilong; Ghaleb, Hesham; Jiang, Yuxuan; Huang, Wenlong; Liu, Yan; Qiu, Qianqian; Qian, Hai published the artcile< Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel>, Electric Literature of 3731-53-1, the main research area is phthalazinone preparation antitumor efflux transporter inhibitor SAR pharmacokinetic; BCRP; Efflux transporter; Multidrug resistance; Oral bioavailability; P-gp.

A series of phthalazinone ring derivatives, I [R = 4-pyridylmethylamino, 2-phenylethylamino, 4-(2-morpholinoethyl)anilino, etc.] with different aromatic heterocycles substituents on the amide bond were designed and synthesized for dual inhibition of P-gp and BCRP. Most target compoundsI significantly increased the accumulation of P-gp substrates in the chemo-resistant cancer cell lines by inhibiting the efflux of transporters. Compound I [R = 4-(2-morpholinoethyl)anilino] in particular showed stronger MDR reversal compared to Gefitinib and Verapamil, and comparable to that of the BCRP inhibitor Ko143. In addition, compound I [R = 4-(2-morpholinoethyl)anilino] improved intestinal absorption of paclitaxel (PTX) and enhanced the bioavailability of the orally administered drug in vivo.

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Electric Literature of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Abas, Mujahid; Nazir, Yasir; Ashraf, Zaman; Iqbal, Zafar; Raza, Hussain; Hassan, Mubashir; Jabeen, Erum; Bais, Abdul published the artcile< A Practical Method of N-Methyl-pyrrole Disulfonamides Synthesis: Computational Studies, Carbonic Anhydrase Inhibition and Electrochemical DNA Binding Investigations>, HPLC of Formula: 3731-53-1, the main research area is methylpyrrole disulfonamide preparation carbonic anhydrase inhibitor antitumor SAR cytotoxicity; mol docking DNA binding.

A series of N-methylpyrrole derivatives bearing disulfonamide functional group, I [R = Bu, Ph, 4-pyridyl, etc.] were synthesized by following a simple nucleophilic substitution reaction route to explore their carbonic anhydrase inhibitory activity. N-methylpyrrole was converted into N-methylpyrrole disulfonyl chloride, which upon condensation with various aliphatic and aromatic amines, yielded the final products I. In-silico docking results predicted strong binding of synthesized compounds I in an enzymic pocket of human carbonic anhydrase isoenzyme II (PDB ID 4Q6D). In-vitro carbonic anhydrase inhibitory assays revealed that analogs I [R = Bu, 2-pyridylethyl] were most potent with IC50 0.38±0.01μM and 0.75±0.88μM resp. in comparison to standard acetazolamide (IC50 0.99±0.04μM). The enzyme inhibitory kinetics exhibited I [R = 2-pyridylethyl] a noncompetitive inhibitor with Km and Ki values as 0.34 mM and 18.2μM resp. The compounds I [R = Bu, 2-pyridylethyl] showed very little cytotoxicity against human keratinocyte (HaCaT) with 80% cell viability and the anticancer activity performed against MCF-7 cell line showed that the compounds I [R = Bu, 2-pyridylethyl] caused 80% and 45% cell death resp. at 125μM concentrations Combining the results of DNA binding anal. through the UV-Vis spectroscopy (hypochromism), cyclic voltammetry (current decrease), and fluorescence spectroscopy (hypochromism in intercalator’s peak); mixed binding mode (intercalation + groove binding) was suggested for I [R = 2-pyridylethyl] and intercalation for I [R = n-butyl] with stronger DNA binding of I [R = 2-pyridylethyl] than I [R = n-butyl]. Based on our results I [R = Bu, 2-pyridylethyl] may be proposed to serve as a lead structure for designing potentially more active CAIs.

ChemistrySelect published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, HPLC of Formula: 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

McCann, Scott D.; Reichert, Elaine C.; Arrechea, Pedro Luis; Buchwald, Stephen L. published the artcile< Development of an Aryl Amination Catalyst with Broad Scope Guided by Consideration of Catalyst Stability>, Recommanded Product: Pyridin-4-ylmethanamine, the main research area is dialkylbiaryl monosphosphine ligand preparation amination coupling catalyst.

The authors have developed a new dialkylbiaryl monophosphine ligand, GPhos, that supports a palladium catalyst capable of promoting carbon-nitrogen cross-coupling reactions between a variety of primary amines and aryl halides; in many cases, these reactions can be carried out at room temperature The reaction development was guided by the idea that the productivity of catalysts employing BrettPhos-like ligands is limited by their lack of stability at room temperature Specifically, it was hypothesized that primary amine and N-heteroaromatic substrates can displace the phosphine ligand, leading to the formation of catalytically dormant palladium complexes that reactivate only upon heating. This notion was supported by the synthesis and kinetic study of a putative off-cycle Pd complex. Consideration of this off-cycle species, together with the identification of substrate classes that are not effectively coupled at room temperature using previous catalysts, led to the design of a new dialkylbiaryl monophosphine ligand. An Ot-Bu substituent was added ortho to the dialkylphosphino group of the ligand framework to improve the stability of the most active catalyst conformer. To offset the increased size of this substituent, the authors also removed the para i-Pr group of the non-phosphorus-containing ring, which allowed the catalyst to accommodate binding of even very large α-tertiary primary amine nucleophiles. In comparison to previous catalysts, the GPhos-supported catalyst exhibits better reactivity both under ambient conditions and at elevated temperatures Its use allows for the coupling of a range of amine nucleophiles, including (1) unhindered, (2) five-membered-ring N-heterocycle-containing, and (3) α-tertiary primary amines, each of which previously required a different catalyst to achieve optimal results.

Journal of the American Chemical Society published new progress about Amination. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Recommanded Product: Pyridin-4-ylmethanamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Valipour, Mehdi; Chippindale, Ann M.; Kouzeli, Aynaz; Irannejad, Hamid published the artcile< A new and facile synthesis of N-benzyl-N'-acylureas via reaction of dibenzoylhydrazine carboxamide and benzylamines>, Application In Synthesis of 3731-53-1, the main research area is benzyl acylurea preparation; dibenzoylhydrazine carboxamide benzylamine amination.

Herein, a new method of synthesis of N-acylureas I (Ar = Ph, 4-methoxyphenyl, 3,4,5-trimethoxyphenyl, pyridin-3-yl, pyridin-4-yl) via reaction of N,2-bis(4-methoxybenzoyl)hydrazine-1-carboxamide and various benzylamines ArCH2NH2 was reported. Preparation of N,2-bis(4-methoxybenzoyl)hydrazine-1-carboxamide was performed by the treatment of 3-methylthio-5,6-bis(4-methoxyphenyl)-1,2,4-triazine with Oxone which leads to oxidation and triazine ring cleavage in high yield (82%). Five benzylamine derivatives I containing different electron donating and withdrawing substituents were used in this study. Yields for the conversion of dibenzoylhydrazine carboxamide to N-acylureas I were in the range of 40-55%.

Synthetic Communications published new progress about Amides Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Application In Synthesis of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem