Category: Pyrazines

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 591-54-8, is researched, Molecular C4H5N3, about Synthesis and anticancer activity of novel Actinonin derivatives as HsPDF inhibitors, the main research direction is peptidomimetic actinonin peptide synthesis antitumor structure activity HsPDF inhibitor; acyl chloride coupling chiral auxiliary alkylation bromoacetate oxidative hydrolysis; aromatic amine coupling proline nucleophilic addition nitrile hydroxylamine cyclization; amide amine peptide coupling hydrolysis Suzuki coupling mol docking; drug design target mechanism action.Formula: C4H5N3.

Human mitochondrial peptide deformylase (HsPDF) is responsible for removing the formyl group from N-terminal formylmethionines of newly synthesized mitochondrial proteins and plays important roles in maintaining mitochondria function. It is overexpressed in various cancers and has been proposed as a novel therapeutic target. Actinonin, a naturally occurring peptidomimetic HsPDF inhibitor, was reported to inhibit the proliferation of a broad spectrum of human cancer cells in vitro. However, its efficacy and pharmacokinetic profile requires significant improvement for therapeutic purposes. To obtain HsPDF inhibitors as anticancer therapeutics, we screened an inhouse collection of actinonin derivatives and found two initial hits with antiproliferation activity. Further optimization along the peptidomimetic backbone lead to two series of compounds containing substituted Ph moieties. They are potent HsPDF inhibitors and exhibited greatly improved antiproliferation activity in selected cancer cell lines. Finally, compound (I) significantly inhibited the growth of human colon cancer in xenograft animal models.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

SDS of cas: 118994-89-1. 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: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Direct C2-Heteroarylation of Indoles by Rhodium-Catalyzed C-C Bond Cleavage of Secondary Alcohols. Author is Yu, Tian-Yang; Zheng, Zhao-Jing; Sun, Wei; Qiao, Zi-Heng.

A rhodium-catalyzed direct heteroarylation of indoles by cleavage of an inert C-C bond of alcs. is reported. This catalytic system exhibits high reactivity and tolerates various functional groups. This reaction provides a tool for the rapid construction of biheteroaryls without pre-activation of the starting materials. Control experiments were conducted to determine a possible mechanism. This reaction makes a significant contribution to the field of C-C bond activation of alcs.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid(SMILESS: O=C(C1N=C(N)SC1)O,cas:2150-55-2) is researched.SDS of cas: 118994-89-1. The article 《Analysis of the cyanide metabolite 2-aminothiazoline-4-carboxylic acid in urine by high-performance liquid chromatography》 in relation to this compound, is published in Analytical Biochemistry. Let’s take a look at the latest research on this compound (cas:2150-55-2).

The cyanide metabolite 2-aminothiazoline-4-carboxylic acid (ATC) was converted to N-carbamylcysteine and analyzed by high-performance liquid chromatog. (HPLC) and fluorometric detection. ATC was first separated from interfering substances by passing through the cation exchanger AG 50W-X8. Interfering disulfides were converted to thiols by reduction of the eluate with thiopropyl-Sepharose 6B. The thiols were then adsorbed to the organomercurial adsorbent p-acetoxymercurianiline-Sepharose 4B while ATC was obtained in the effluent. ATC was then converted to N-carbamylcysteine by ring opening at high temperature in an alk. environment. Derivatization of N-carbamylcysteine was with N-(7-dimethylamino-4-methyl-3-coumarinyl)maleimide. The imprecision (CV) of the method was 3.6% and the anal. recovery was quant. The detection limit was 0.3 μM. ATC in urine was stable for at least 3 mo when stored at -196 to +20 °C. The ATC concentration in urine was below the limit of detection in healthy nonsmokers. The utility of the method was demonstrated by the finding of up to 10.5 μM ATC concentrations in urine samples from human subjects in Mozambique living on a high dietary intake of cyanide from the cassava root. In a metabolic study rats were exposed to acetonitrile in the drinking water. After 4 wk very high ATC levels were found in the urine, representative values from two rats being 195 and 525 μM, resp.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of 4-Aminopyrimidine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Racemization-free synthesis of dipeptide, amide and ester by oxalyl chloride and catalytic triphenylphosphine oxide. Author is Ren, Ji-Wei; Tong, Meng-Nan; Zhao, Yu-Fen; Ni, Feng.

An efficient triphenylphosphine oxide (Ph3PO) catalyzed amidation and esterification reaction for rapid synthesis of a series of dipeptides, amides and esters under mild condition is described. This reaction is applicable to challenging couplings of hindered carboxylic acid with low nucleophilic amine or alc., giving products in good yields (67-90%) without any racemization. This system employs highly reactive intermediate Ph3PCl2 as activator of carboxylate, in a catalytic manner, and drive the reaction to complete in short reaction time (less than 10 min). It has the advantages of good functional group tolerance, broad substrate scope and good atom-economy. A 100 mmol scale reaction with good yield shed light on its potential for industrial application. A plausible mechanism is proposed based on 31P NMR monitor of reaction process.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

HPLC of Formula: 118994-89-1. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Total synthesis of potent antifungal marine bisoxazole natural products benzazoles A and B. Author is Bull, James A.; Balskus, Emily P.; Horan, Richard A. J.; Langner, Martin; Ley, Steven V..

The bengazoles are a family of marine natural products that display potent antifungal activity and a unique structure, containing two oxazole rings flanking a single carbon atom. Total syntheses of benzazole A and B are described, which contain a sensitive stereogenic center at this position between the two oxazoles. Addnl., the synthesis of 10-epi-benzazole A is reported. Two parallel synthetic routes were investigated, relying on construction of the 2,4-disubstituted oxazole under mild conditions and a diastereoselective 1,3-dipolar cycloaddition Our successful route is high yielding, provides rapid access to single stereoisomers of the complex natural products and allows the synthesis of analogs for biol. evaluation.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

COA of Formula: C4H5N3. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Reductive Amination Revisited: Reduction of Aldimines with Trichlorosilane Catalyzed by Dimethylformamide – Functional Groups Tolerance, Scope, and Limitations. Author is Popov, Kirill K.; Campbell, Joanna L. P.; Kysilka, Ondrej; Hosek, Jan; Davies, Christopher D.; Pour, Milan; Kocovsky, Pavel.

Aldimines R1CH2NHR2 (R1 = but-3-yn-1-yl, Ph, thiophen-2-yl, etc.; R2 = Bu, Bn, cyclohexyl, 5-methyl-1,3,4-thiadiazol-2-yl, etc.), generated in situ from aliphatic, aromatic, and heteroaromatic aldehydes R1CHO and aliphatic, aromatic, and heteroaromatic primary or secondary amines R2NH2, can be reduced with trichlorosilane in the presence of DMF (DMF) as an organocatalyst (≤10 mol%) in toluene or CH2Cl2 at room temperature The reduction tolerates ketone carbonyls, esters, amides, nitriles, sulfones, sulfonamides, NO2, SF5, and CF3 groups, boronic esters, azides, phosphine oxides, C=C and CC bonds, and ferrocenyl nucleus but sulfoxides and N-oxides are reduced. α,β-Unsaturated aldimines undergo 1,2-reduction only, leaving the C=C bond intact. N-Monoalkylation of primary amines is attained with a 1:1 aldehyde to amine ratio, whereas excess of the aldehyde (≥2:1) allows second alkylation, giving rise to tertiary amines. Reductive N-alkylation of α-amino acids proceeds without racemization; the resulting products, containing a CC bond or N3 group, are suitable for click chem. This reaction thus offers advantages over the traditional methods (borohydride reduction or catalytic hydrogenation) in terms of efficiency and chemoselectivity. Solubility of some of the reacting partners appears to be the only limitation. The byproducts generated by the workup with aqueous NaHCO3 (i.e., NaCl and silica) are environmentally benign. As a greener alternative, DMA can be employed as a catalyst instead of DMF.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Recommanded Product: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid. 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: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Analysis of the cyanide metabolite 2-aminothiazoline-4-carboxylic acid in urine by high-performance liquid chromatography. Author is Lundquist, Per; Kagedal, Bertil; Nilsson, Lennart; Rosling, Hans.

The cyanide metabolite 2-aminothiazoline-4-carboxylic acid (ATC) was converted to N-carbamylcysteine and analyzed by high-performance liquid chromatog. (HPLC) and fluorometric detection. ATC was first separated from interfering substances by passing through the cation exchanger AG 50W-X8. Interfering disulfides were converted to thiols by reduction of the eluate with thiopropyl-Sepharose 6B. The thiols were then adsorbed to the organomercurial adsorbent p-acetoxymercurianiline-Sepharose 4B while ATC was obtained in the effluent. ATC was then converted to N-carbamylcysteine by ring opening at high temperature in an alk. environment. Derivatization of N-carbamylcysteine was with N-(7-dimethylamino-4-methyl-3-coumarinyl)maleimide. The imprecision (CV) of the method was 3.6% and the anal. recovery was quant. The detection limit was 0.3 μM. ATC in urine was stable for at least 3 mo when stored at -196 to +20 °C. The ATC concentration in urine was below the limit of detection in healthy nonsmokers. The utility of the method was demonstrated by the finding of up to 10.5 μM ATC concentrations in urine samples from human subjects in Mozambique living on a high dietary intake of cyanide from the cassava root. In a metabolic study rats were exposed to acetonitrile in the drinking water. After 4 wk very high ATC levels were found in the urine, representative values from two rats being 195 and 525 μM, resp.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of 5-Amino-2-fluoropyridine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Copper-Catalyzed Electrochemical C-H Amination of Arenes with Secondary Amines. Author is Yang, Qi-Liang; Wang, Xiang-Yang; Lu, Jia-Yan; Zhang, Li-Pu; Fang, Ping; Mei, Tian-Sheng.

Electrochem. oxidation represents an environmentally friendly solution to conventional methods that require caustic stoichiometric chem. oxidants. However, C-H functionalizations merging transition-metal catalysis and electrochem. techniques are, to date, largely confined to the use of precious metals and divided cells. Herein, the authors report the 1st examples of Cu-catalyzed electrochem. C-H aminations of arenes at room temperature using undivided electrochem. cells, thereby providing a practical solution for the construction of arylamines. The use of Bu4NI as a redox mediator is crucial for this transformation. From mechanistic studies including kinetic profiles, isotope effects, cyclic voltammetric analyses, and radical inhibition experiments, the reaction appears to proceed via a single-electron-transfer (SET) process, and a high valent Cu(III) species is likely involved. These findings provide a new avenue for transition-metal-catalyzed electrochem. C-H functionalization reactions using redox mediators.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《4,6-Dichloro- and 4,5,6-trichloropicolinic acid》. Authors are Graf, Roderich.The article about the compound:3-Chloropicolinamidecas:114080-95-4,SMILESS:O=C(N)C1=NC=CC=C1Cl).HPLC of Formula: 114080-95-4. Through the article, more information about this compound (cas:114080-95-4) is conveyed.

cf. C. A. 25, 2428. Picolinic acid-HCl (200 g.) and 350 cc. SOCl2, gently boiled 10 days, give 30 g. mono-Cl acid, 100 g. di-Cl acid and 30 g. of a mixture of the di- and tri-Cl acids. That the di-Cl acid is the 4,6-Cl2 derivative is shown by the following reactions: The acid chloride and N2H4.H2O in C6H6 give sec-bis(4,6-dichloropicolinic acid) hydrazide, m. above 300°; the Me ester gives 4,6-dichloropicolinic acid hydrazide, m. 154° (benzal derivative, m. 165°); the azide m. 74° and with absolute EtOH yields 4,6-di-chloro-2-carbethoxypyridine, m. 75°; dilute AcOH gives the 2-NH2 derivative (I), m. 108°; with HI I yields a compound, m. 137°, which may be the 6-iodo-4-chloro derivative The Ac derivative of I n. 218-9°. The diazo solution from I in H2SO4 gives 4,6-dichloro-2-hydroxy-pyridine, m. 151°, and in concentrated HCl gives 2,4,6-trichloropyridine, m. 33°; this also results from 2,6-dichloro-4-aminopyridine. Heating the 4,6-Cl2 acid with 80% H2SO4 8 hrs. gives 4-chloro-6-hydroxypicolinic acid (Seyfferth, J. Chem. Soc. 67, 408(1895). 4,5,6-Trichloropicolinic acid (II), crystallizing with 1 mol. H2O, m. 123°, is obtained pure by distillation of the chloride and then of the Me ester, m. 125°; II and HI with some red P, heated 8 hrs. at 150°, give 5-chloropicolinic acid, m. 170°. The amide of II m. 169°; the Ph ester m. 138°. Heating the Me ester with HI and red P 5 hrs. gives 4-iodo-5-chloropicolinic acid, m. 159° (decomposition); refluxed with SOCl2 for 4 hrs., the I is replaced by Cl, giving 4,5-dichloropicolinic acid, crystals with 1 mol. H2O, m. 179-80° (Ost, J. prakt. Chem. 27, 274(1882)). Refluxing the Me ester with 80% H2SO4 4 hrs. gives 4,5-dichloro-6-hydroxypicolinic acid, crystallizing with 1 mol. H2O, m. 284° (decomposition). 3-Chloropicolinic acid, m. 121°; amide, m. 140°.

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Pyrazine – Wikipedia,
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SDS of cas: 591-54-8. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites. Author is 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..

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,
Pyrazine | C4H4N2 – PubChem