Category: 591-54-8

Jiang, Yong; Hu, Miao; Sun, Nan; Hu, Baoxiang; Shen, Zhenlu; Hu, Xinquan; Jin, Liqun published the article 《Bidentate geometry-constrained iminopyridyl nickel-catalyzed synthesis of amines or imines via borrowing hydrogen or dehydrogenative condensation》. Keywords: secondary amine preparation; primary amine alc iminopyridyl nickel catalyst alkylation; imine preparation; alkyl amine alc iminopyridyl nickel catalyst dehydrogenative coupling reaction; bidentate geometry constrained iminopyridyl nickel catalyst preparation.They researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Application In Synthesis of 4-Aminopyrimidine. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:591-54-8) here.

The efficient Ni-catalyzed N-alkylation of various anilines with alcs. via borrowing hydrogen was reported using a bidentate geometry-constrained iminopyridyl nickel complex as the catalyst. Substituted benzylic alcs. and short/long chain aliphatic alcs. could be applied as the alkylation sources to couple with aromatic and heteroaromatic amines to give a diverse set of N-alkylation outcomes in moderate to excellent yields. The nickel catalytic system was also suitable for aliphatic amines, selectively delivering the corresponding imines via an acceptorless dehydrogenative condensation strategy.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Aminopyrimidine( cas:591-54-8 ) is researched.Related Products of 591-54-8.Chen, Ying-Chu; Faver, John C.; Ku, Angela F.; Miklossy, Gabriella; Riehle, Kevin; Bohren, Kurt M.; Ucisik, Melek N.; Matzuk, Martin M.; Yu, Zhifeng; Simmons, Nicholas published the article 《C-N Coupling of DNA-Conjugated (Hetero)aryl Bromides and Chlorides for DNA-Encoded Chemical Library Synthesis》 about this compound( cas:591-54-8 ) in Bioconjugate Chemistry. Keywords: DNA encoded heteroaryl amide library synthesis. Let’s learn more about this compound (cas:591-54-8).

DNA-encoded chem. library (DECL) screens are a rapid and economical tool to identify chem. starting points for drug discovery. As a robust transformation for drug discovery, palladium-catalyzed C-N coupling is a valuable synthetic method for the construction of DECL chem. matter; however, currently disclosed methods have only been demonstrated on DNA-attached (hetero)aromatic iodide and bromide electrophiles. We developed conditions utilizing an N-heterocyclic carbene-palladium catalyst that extends this reaction to the coupling of DNA-conjugated (hetero)aromatic chlorides with (hetero)aromatic and select aliphatic amine nucleophiles. In addition, we evaluated steric and electronic effects within this catalyst series, carried out a large substrate scope study on two representative (hetero)aryl bromides, and applied this newly developed method within the construction of a 63 million-membered DECL.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Development of an Aryl Amination Catalyst with Broad Scope Guided by Consideration of Catalyst Stability, the main research direction is dialkylbiaryl monosphosphine ligand preparation amination coupling catalyst.Product Details of 591-54-8.

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.

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Related Products of 591-54-8. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Boramidine: A Versatile Structural Motif for the Design of Fluorescent Heterocycles. Author is Lebedev, Yury; Apte, Chirag; Cheng, Susan; Lavigne, Cyrille; Lough, Alan; Aspuru-Guzik, Alan; Seferos, Dwight S.; Yudin, Andrei K..

Sodium cyanoborohydride-derived N-alkylnitriliumboranes were found to be versatile precursors for the synthesis of novel boron-containing heterocycles. The reaction between N-alkylnitriliumboranes and 2-aminopyridines, -imidazoles, -oxazoles, or -isoxazoles leads to incorporation of the [B-C] motif into a five-membered boramidine which exist as a mixture of Z and E isomers. The resulting heterocycles are blue-fluorescent in both the solid state and in solution with ca. 2700 – 8400 cm-1 Stokes shifts and quantum yields in the 65 – 74% range in water and in the 42 – 84% range in organic solvents. The combination of photophys. properties, structural tunability, stability, and solubility in various media are expected to find application in a range of disciplines.

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Safety of 4-Aminopyrimidine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Design, synthesis and biological evaluation of pyrazole-aromatic containing carboxamides as potent SDH inhibitors.

To continue studies on discovery of new potent antifungal leads, 43 novel pyrazole-aromatic containing carboxamides were rationally designed and synthesized. Bioassays indicated that most target compounds displayed good in vitro antifungal activities against Botrytis cinerea, Rhizoctonia cerealis and Sclerotinia sclerotiorum and in vivo antifungal activity against R. solani. Compound I exhibited the most significant in vitro activity against R. cerealis (EC50 = 0.93μg/mL) with about 2-fold more potent than a previously reported lead compound N-(3-bromophenyl)-2-[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]-4-thiazolecarboxamide (EC50 = 2.01μg/mL), and about 11-fold more potent than the pos. control/com. succinate dehydrogenase inhibitor thifluzamide (EC50 = 23.09μg/mL). Structure-activity relationship anal. and mol. docking simulations indicated that the presence of difluoromethyl pyrazole-(m-benzene)carboxamide scaffold obviously increased the antifungal activity. The further enzymic bioassay showed that both thifluzamide and compound I displayed excellent SDH inhibitory effects, and fluorescence quenching anal. suggested that they may share the same target SDH.

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Song, Di; Zhang, Nan; Zhang, Panpan; Zhang, Na; Chen, Weijin; Zhang, Long; Guo, Ting; Gu, Xiaotong; Ma, Shutao published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).Product Details of 591-54-8. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:591-54-8) through the article.

With the increasing incidence of antibiotic resistance, new antibacterial agents having novel mechanisms of action hence are in an urgent need to combat infectious diseases caused by multidrug-resistant (MDR) pathogens. Four novel series of substituted 9-arylalkyl-10-methylacridinium derivatives as FtsZ inhibitors were designed, synthesized and evaluated for their antibacterial activities against various Gram-pos. and Gram-neg. bacteria. The results demonstrated that they exhibited broad-spectrum activities with substantial efficacy against MRSA and VRE, which were superior or comparable to the berberine, sanguinarine, linezolid, ciprofloxacin and vancomycin. In particular, the most promising compound I showed rapid bactericidal properties, which avoid the emergence of drug resistance. However, I showed no inhibitory effect on Gram-neg. bacteria but biofilm formation study gave possible answers. Further target identification and mechanistic studies revealed that I functioned as an effective FtsZ inhibitor to alter the dynamics of FtsZ self-polymerization, which resulted in termination of the cell division and caused cell death. Further cytotoxicity and animal studies demonstrated that I not only displayed efficacy in a murine model of bacteremia in vivo, but also no significant hemolysis to mammalian cells. Overall, this compound with novel skeleton could serve as an antibacterial lead of FtsZ inhibitor for further evaluation of drug-likeness.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Matralis, Alexios N.; Malik, Adnan; Penzo, Maria; Moreno, Inmaculada; Almela, Maria J.; Camino, Isabel; Crespo, Benigno; Saadeddin, Anas; Ghidelli-Disse, Sonja; Rueda, Lourdes; Calderon, Felix; Osborne, Simon A.; Drewes, Gerard; Boesche, Markus; Fernandez-Alvaro, Elena; Martin Hernando, Jose Ignacio; Baker, David A. researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).SDS of cas: 591-54-8.They published the article 《Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites》 about this compound( cas:591-54-8 ) in Journal of Medicinal Chemistry. Keywords: Plasmodium malaria PKG inhibitor fast killing SRPK2 antimalarial. We’ll tell you more about this compound (cas:591-54-8).

One of the attractive properties of artemisinins is their extremely fast-killing capability, quickly relieving malaria symptoms. Nevertheless, the unique benefits of these medicines are now compromised by the prolonged parasite clearance times and the increasing frequency of treatment failures, attributed to the increased tolerance of Plasmodium falciparum to artemisinin. This emerging artemisinin resistance threatens to undermine the effectiveness of antimalarial combination therapies. Herein, we describe the medicinal chem. efforts focused on a cGMP-dependent protein kinase (PKG) inhibitor scaffold, leading to the identification of novel chem. entities with very potent, similar to artemisinins, fast-killing potency against asexual blood stages that cause disease, and activity against gametocyte activation that is required for transmission. Furthermore, we confirm that selective PKG inhibitors have a slow speed of kill, while chemoproteomic anal. suggests for the first time serine/arginine protein kinase 2 (SRPK2) targeting as a novel strategy for developing antimalarial compounds with extremely fast-killing properties.

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Pyrazine – Wikipedia,
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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Aminopyrimidine( cas:591-54-8 ) is researched.Safety of 4-Aminopyrimidine.Chen, Zhixiang; Ma, Dawei published the article 《Cu/N,N’-Dibenzyloxalamide-Catalyzed N-Arylation of Heteroanilines》 about this compound( cas:591-54-8 ) in Organic Letters. Keywords: aryl halide heteroarylamine arylation copper oxalamide; diarylamine preparation; copper oxalamide arylation catalyst. Let’s learn more about this compound (cas:591-54-8).

N,N’-Dibenzyloxalamide (DBO) was identified as a powerful ligand for promoting Cu-catalyzed coupling of heteroanilines with (hetero)aryl halides. For (hetero)aryl chlorides, the coupling reaction occurred at 130 °C with 5 mol % CuBr and 10 mol % DBO. For (hetero)aryl bromides/iodides, coupling reaction took place at 80-100 °C with 1 mol % CuI and 2 mol % DBO. A variety of heteroanilines worked well to afford the arylation products in good to excellent yields.

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Pyrazine – Wikipedia,
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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Lebedev, Yury; Apte, Chirag; Cheng, Susan; Lavigne, Cyrille; Lough, Alan; Aspuru-Guzik, Alan; Seferos, Dwight S.; Yudin, Andrei K. researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Product Details of 591-54-8.They published the article 《Boramidine: A Versatile Structural Motif for the Design of Fluorescent Heterocycles》 about this compound( cas:591-54-8 ) in Journal of the American Chemical Society. Keywords: Boramidine fluorescence heterocycle. We’ll tell you more about this compound (cas:591-54-8).

Sodium cyanoborohydride-derived N-alkylnitriliumboranes were found to be versatile precursors for the synthesis of novel boron-containing heterocycles. The reaction between N-alkylnitriliumboranes and 2-aminopyridines, -imidazoles, -oxazoles, or -isoxazoles leads to incorporation of the [B-C] motif into a five-membered boramidine which exist as a mixture of Z and E isomers. The resulting heterocycles are blue-fluorescent in both the solid state and in solution with ca. 2700 – 8400 cm-1 Stokes shifts and quantum yields in the 65 – 74% range in water and in the 42 – 84% range in organic solvents. The combination of photophys. properties, structural tunability, stability, and solubility in various media are expected to find application in a range of disciplines.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Matralis, Alexios N.; Malik, Adnan; Penzo, Maria; Moreno, Inmaculada; Almela, Maria J.; Camino, Isabel; Crespo, Benigno; Saadeddin, Anas; Ghidelli-Disse, Sonja; Rueda, Lourdes; Calderon, Felix; Osborne, Simon A.; Drewes, Gerard; Boesche, Markus; Fernandez-Alvaro, Elena; Martin Hernando, Jose Ignacio; Baker, David A. published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).Application of 591-54-8. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:591-54-8) through the article.

One of the attractive properties of artemisinins is their extremely fast-killing capability, quickly relieving malaria symptoms. Nevertheless, the unique benefits of these medicines are now compromised by the prolonged parasite clearance times and the increasing frequency of treatment failures, attributed to the increased tolerance of Plasmodium falciparum to artemisinin. This emerging artemisinin resistance threatens to undermine the effectiveness of antimalarial combination therapies. Herein, we describe the medicinal chem. efforts focused on a cGMP-dependent protein kinase (PKG) inhibitor scaffold, leading to the identification of novel chem. entities with very potent, similar to artemisinins, fast-killing potency against asexual blood stages that cause disease, and activity against gametocyte activation that is required for transmission. Furthermore, we confirm that selective PKG inhibitors have a slow speed of kill, while chemoproteomic anal. suggests for the first time serine/arginine protein kinase 2 (SRPK2) targeting as a novel strategy for developing antimalarial compounds with extremely fast-killing properties.

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Pyrazine – Wikipedia,
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