Month: October 2022

Reference of 1H-Imidazol-2-amineIn 2021 ,《Synthesis and molecular docking of some new 3,5-bis-(diazepine, pyrazolopyrimidine, pyrimidine, and pyrazole) pyridine derivatives and their in vitro and in vivo biological evaluation as potential antitumor agents》 appeared in Journal of Heterocyclic Chemistry. The author of the article were Soliman, Nanees N.; Tag, Yasmin M.; Bayoumy, Nesma M.. The article conveys some information:

Dihydropyridine-containing bisenaminone I was used to synthesize new heterocyclic compounds containing nitrogen moieties, such as II (R = H, Me, Ph, H2N, 6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl) by reaction with different bifunctional reagents. Moreover, the new compounds were screened in vitro as antitumor agents for Ehrlich ascites at different concentrations The results showed that selected compounds such as II (R = H) had good activity. In addition the mol. docking of these mentioned compounds was studied using vascular endothelial growth factor receptor. In addition to this study using 1H-Imidazol-2-amine, there are many other studies that have used 1H-Imidazol-2-amine(cas: 7720-39-0Reference of 1H-Imidazol-2-amine) was used in this study.

1H-Imidazol-2-amine(cas: 7720-39-0) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Reference of 1H-Imidazol-2-amine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Recommanded Product: 58-85-5In 2020 ,《Biotin synthesis in Ralstonia eutropha H16 utilizes pimeloyl coenzyme A and can be regulated by the amount of acceptor protein》 appeared in Applied and Environmental Microbiology. The author of the article were Eggers, Jessica; Strittmatter, Carl Simon; Kuesters, Kira; Biller, Emre; Steinbuechel, Alexander. The article conveys some information:

The biotin metabolism of the Gram-neg. facultative chemolithoautotrophic bacterium Ralstonia eutropha (syn. Cupriavidus necator), which is used for biopolymer production in industry, was investigated. A biotin auxotroph mutant lacking bioF was generated, and biotin depletion in the cells and the minimal biotin demand of a biotin-auxotrophic R. eutropha strain were determined Three consecutive cultivations in biotin-free medium were necessary to prevent growth of the auxotrophic mutant, and 40 ng/mL biotin was sufficient to promote cell growth. Nevertheless, 200 ng/mL biotin was necessary to ensure growth comparable to that of the wild type, which is similar to the demand of biotin-auxotrophic mutants among other prokaryotic and eukaryotic microbes. A phenotypic complementation of the R. eutropha ΔbioF mutant was only achieved by homologous expression of bioF of R. eutropha or heterologous expression of bioF of Bacillus subtilis but not by bioF of Escherichia coli. Together with the results from bioinformatic anal. of BioFs, this leads to the assumption that the intermediate of biotin synthesis in R. eutropha is pimeloyl-CoA instead of pimeloyl-acyl carrier protein (ACP) like in the Gram-pos. B. subtilis. Internal biotin content was enhanced by homologous expression of accB, whereas homologous expression of accB and accC2 in combination led to decreased biotin concentrations in the cells. Although a DNA-binding domain of the regulator protein BirA is missing, biotin synthesis seemed to be influenced by the amount of acceptor protein present. The experimental part of the paper was very detailed, including the reaction process of 5-((3aS,4S,6aR)-2-Oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoic acid(cas: 58-85-5Recommanded Product: 58-85-5)

5-((3aS,4S,6aR)-2-Oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoic acid(cas: 58-85-5) may be used to elute proteins from avidin/streptavidin resins. It has been used for culturing of oligodendrocytes.Recommanded Product: 58-85-5 And it has been used as a vitamin supplement for the growth of Bacillus species.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Electric Literature of C7H7N3In 2020 ,《Copper-Catalyzed Synthesis of Trinuclear N-Fused Hybrid Scaffolds by Double C(sp2)-N Bond Formation between 2-(2-Bromoaryl)indoles and 2-Aminoazoles》 appeared in European Journal of Organic Chemistry. The author of the article were Diep, Thi Duyen; Pham, Duy Quang Dao; Ho, Son Long; Cho, Chan Sik. The article conveys some information:

2-(2-Bromoaryl)indoles react with 2-aminoazoles by microwave irradiation in DMF in the presence of a catalytic amount of CuI and a base to produce trinuclear N-fused hybrid scaffolds, benzo[4,5]imidazo[1,2-a]indolo[1,2-c]quinazolines and imidazo[1,2-a]indolo[1,2-c]quinazolines in moderate to good yields [e.g., 2-(2-bromophenyl)indole + 2-aminobenzimidazole → I (74%) in presence of CuI and K3PO4 in DMF]. The reaction seems to proceed via copper-catalyzed C(sp2)-N coupling and subsequent intramol. cyclocondensation accompanied by ammonia evolution. Complete regioselective C-N cyclization is observed with the reaction of 2-(2-bromophenyl)indole with 2-aminoazoles. In the part of experimental materials, we found many familiar compounds, such as 1H-Benzo[d]imidazol-2-amine(cas: 934-32-7Electric Literature of C7H7N3)

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.Electric Literature of C7H7N3

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Category: imidazoles-derivativesIn 2019 ,《Green, effective and chromatography free synthesis of benzoimidazo[1,2-a]pyrimidine and tetrahydrobenzo [4,5]imidazo [1,2-d]quinazolin-1(2H)-one and their pyrazolyl moiety using Fe3O4@SiO2@L-proline reusable catalyst in aqueous media》 appeared in Journal of Organometallic Chemistry. The author of the article were Fekri, Leila Zare; Nikpassand, Mohammad; Khakshoor, Samira Nazari. The article conveys some information:

L-proline-functionalized silica-coated Fe3O4 nanoparticle was synthesized and characterized using Fourier Transform IR spectroscopy, X-ray diffraction, field emission SEM, transmission electron microscopy, energy dispersive X-ray spectroscopy, thermogravimetric anal., Zeta potential and a vibrating sample magnetometer. The Fe3O4@SiO2@L-proline nanoparticles in aqueous media were used as a green avenue for the mild and efficient multicomponent synthesis of new derivatives of benzoimidazo[1,2-a]pyrimidines and tetrahydrobenzo[4,5]imidazo-[1,2-d]quinazolin-1(2H)-ones in excellent yields. Furthermore, the recovery and reuse of the catalyst was demonstrated 10 times without a detectable loss in activity. Eco-friendliness, high purity of the desired products, short reaction time and easy workup was mentioned as the other advantages of this method. The results came from multiple reactions, including the reaction of 1H-Benzo[d]imidazol-2-amine(cas: 934-32-7Category: imidazoles-derivatives)

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Recommanded Product: 1,3-Dimesityl-1H-imidazol-3-ium chlorideIn 2022 ,《Ruthenium complexes with chelating carboxylate-NHC ligands as efficient catalysts for C-H arylation in water》 was published in Mendeleev Communications. The article was written by Shepelenko, Konstantin E.; Nikolaeva, Ksenia A.; Shevchenko, Maxim A.; Tkachenko, Yurii N.; Minyaev, Mikhail E.; Chernyshev, Victor M.. The article contains the following contents:

Ruthenium(II) complexes [(p-cymene)RuCl(3-R-Im-1-CH2CO2)] (1a-c, H2Im = 2-imidazolylidene; R = Me, Mes, Dipp), [(p-cymene)RuCl(3-R1-Im-1-CH2CONR2)] (2a-d; R1 = Me, Mes, Dipp; R2 = Dipp, tBu, Mes) with chelating N-heterocyclic carbene (NHC) ligands functionalized with carboxy and carboxamidato pendant groups, were prepared and examined as catalysts for ortho-C-H arylation of Ph groups in 2-phenylpyridine and 1-phenylpyrazole with aryl chlorides in water affording substituted 2-(m-terphenylyl)pyridines and 1-(m-terphenylyl)pyrazoles. Complexes with NHC-ligands containing a hemilabile coordinating N-carboxylatomethyl group enable fast and selective ortho-CH-diarylation in the absence of carboxylate-assisting additives. In the experimental materials used by the author, we found 1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8Recommanded Product: 1,3-Dimesityl-1H-imidazol-3-ium chloride)

1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8) is a ligand for arylation of aldehydes and for carbene catalyzed intermolecular arylation of C-H bonds. It is used as a phosphine-free ligand in various metal-catalyzed coupling reactions, often with advantageous results in difficult cases.Recommanded Product: 1,3-Dimesityl-1H-imidazol-3-ium chloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Related Products of 530-62-1In 2019 ,《Harnessing Secondary Coordination Sphere Interactions That Enable the Selective Amidation of Benzylic C-H Bonds》 was published in Journal of the American Chemical Society. The article was written by Jung, Hoimin; Schrader, Malte; Kim, Dongwook; Baik, Mu-Hyun; Park, Yoonsu; Chang, Sukbok. The article contains the following contents:

Engineering site-selectivity is highly desirable especially in C-H functionalization reactions. We report a new catalyst platform that is highly selective for the amidation of benzylic C-H bonds controlled by π-π interactions in the secondary coordination sphere. Mechanistic understanding of the previously developed iridium catalysts that showed poor regioselectivity gave rise to the recognition that the π-cloud of an aromatic fragment on the substrate can act as a formal directing group through an attractive noncovalent interaction with the bidentate ligand of the catalyst. On the basis of this mechanism-driven strategy, we developed a cationic (η5-C5H5)Ru(II) catalyst with a neutral polypyridyl ligand to obtain record-setting benzylic selectivity in an intramol. C-H lactamization in the presence of tertiary C-H bonds at the same distance. Exptl. and computational techniques were integrated to identify the origin of this unprecedented benzylic selectivity, and robust linear free energy relationship between solvent polarity index and the measured site-selectivity was found to clearly corroborate that the solvophobic effect drives the selectivity. Generality of the reaction scope and applicability toward versatile γ-lactam synthesis were demonstrated.Di(1H-imidazol-1-yl)methanone(cas: 530-62-1Related Products of 530-62-1) was used in this study.

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a coupling agent in the synthesis of dipolar polyamides for nonlinear optical applications and polypeptides. It also used to make β-keto sulfones and sulfoxides, lead sequestering agents, and β-enamino acid derivatives.Related Products of 530-62-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Related Products of 141556-45-8In 2022 ,《Antileishmanial activity and insights into the mechanisms of action of symmetric Au(I) benzyl and aryl-N-heterocyclic carbenes》 was published in Journal of Inorganic Biochemistry. The article was written by Rosa, Leticia B.; Galuppo, Carolina; Lima, Rochanna L. A.; Fontes, Josielle V.; Siqueira, Fabio S.; Judice, Wagner A. S.; Abbehausen, Camilla; Miguel, Danilo C.. The article contains the following contents:

Leishmania amazonensis and L. braziliensis are the main etiol. agents of the American Tegumentary Leishmaniasis (ATL). Taking into account the limited effectiveness and high toxicity of the current drug arsenal to treat ATL, novel options are urgently needed. Inspired by the fact that gold-based compounds are promising candidates for antileishmanial drugs, we studied the biol. action of a systematic series of six (1)-(6) sym. Au(I) benzyl and aryl-N-heterocyclic carbenes. All compounds were active at low micromolar concentrations with 50% effective concentrations ranging from 1.57 to 8.30 μM against Leishmania promastigotes. The mesityl derivative (3) proved to be the best candidate from this series, with a selectivity index ∼13 against both species. The results suggest an effect of the steric and electronic parameters of the N-substituent in the activity. Intracellular infections were drastically reduced after 24h of (2)-(5) incubation in terms of infection rate and amastigote burden. Further investigations showed that our compounds induced significant parasites′ morphol. alterations and membrane permeability. Also, (3) and (6) were able to reduce the residual activity of three Leishmania recombinant cysteine proteases, known as possible targets for Au(I) complexes. Our promising results open the possibility of exploring gold complexes as leishmanicidal mols. to be further screened in in vivo models of infection.1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8Related Products of 141556-45-8) was used in this study.

1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8) is a ligand for arylation of aldehydes and for carbene catalyzed intermolecular arylation of C-H bonds. It is used as a phosphine-free ligand in various metal-catalyzed coupling reactions, often with advantageous results in difficult cases.Related Products of 141556-45-8

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《NHC-Catalyzed Oxidative Annulation of α,β-unsaturated Aldehydes with Benzyl Ketones: Direct Access to 4,5,6-Trisubstituted Dihydropyranones》 was written by Wang, Zhan-Yong; Liu, Qingling; Wang, Kai-Kai; Liu, Menghan; Han, Yafei; Sun, Aili; Ma, Xueji. Application of 141556-45-8This research focused ontrisubstituted dihydropyranone preparation green chem; unsaturated aldehyde benzyl ketone oxidative cyclization NHC catalyst. The article conveys some information:

A novel and efficient access to polysubstituted dihydropyranones I (R = Ph, 4-MeOC6H4, 2-furyl, n-Pr, etc.; Ar = Ph, 4-MeC6H4, 4-ClC6H4; Ar1 = Ph, 2-naphthyl, 4-NCC6H4, etc.) was developed by N-heterocyclic carbene catalyzed annulation reaction of α,β-unsaturated aldehydes and benzyl ketones under oxidative conditions. Various α,β-unsaturated aldehydes with long-chain aliphatic and aromatic substitution groups were compatible in this transformation, giving the corresponding products in good to excellent yields under mild conditions. This strategy features simple and readily available materials and mild reaction conditions and provides a green and practical method for the rapid synthesis of functionalized dihydropyranones. In the experiment, the researchers used 1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8Application of 141556-45-8)

1,3-Dimesityl-1H-imidazol-3-ium chloride(cas: 141556-45-8) is a ligand for arylation of aldehydes and for carbene catalyzed intermolecular arylation of C-H bonds. It is used as a phosphine-free ligand in various metal-catalyzed coupling reactions, often with advantageous results in difficult cases.Application of 141556-45-8

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition》 was written by Reich, Siegfried H.; Sprengeler, Paul A.; Chiang, Gary G.; Appleman, James R.; Chen, Joan; Clarine, Jeff; Eam, Boreth; Ernst, Justin T.; Han, Qing; Goel, Vikas K.; Han, Edward Z. R.; Huang, Vera; Hung, Ivy N. J.; Jemison, Adrianna; Jessen, Katti A.; Molter, Jolene; Murphy, Douglas; Neal, Melissa; Parker, Gregory S.; Shaghafi, Michael; Sperry, Samuel; Staunton, Jocelyn; Stumpf, Craig R.; Thompson, Peggy A.; Tran, Chinh; Webber, Stephen E.; Wegerski, Christopher J.; Zheng, Hong; Webster, Kevin R.. Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile And the article was included in Journal of Medicinal Chemistry on April 26 ,2018. The article conveys some information:

Dysregulated translation of mRNA plays a major role in tumorigenesis. Mitogen-activated protein kinase interacting kinases (MNK)1/2 are key regulators of mRNA translation integrating signals from oncogenic and immune signaling pathways through phosphorylation of eIF4E and other mRNA binding proteins. Modulation of these key effector proteins regulates mRNA, which controls tumor/stromal cell signaling. Compound 23 (eFT508, 6′-((6-aminopyrimidin-4-yl)amino)-8′-methyl-2’H-spiro-[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione hydrochloride), an exquisitely selective, potent dual MNK1/2 inhibitor, was designed to assess the potential for control of oncogene signaling at the level of mRNA translation. The crystal structure-guided design leverages stereoelectronic interactions unique to MNK culminating in a novel pyridone-aminal structure described for the first time in the kinase literature. Compound 23 has potent in vivo antitumor activity in models of diffuse large cell B-cell lymphoma and solid tumors, suggesting that controlling dysregulated translation has real therapeutic potential. Compound 23 is currently being evaluated in Phase 2 clin. trials in solid tumors and lymphoma. Compound 23 is the first highly selective dual MNK inhibitor targeting dysregulated translation being assessed clin. In the experiment, the researchers used many compounds, for example, Imidazo[1,2-a]pyridine-8-carbonitrile(cas: 136117-70-9Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile)

Imidazo[1,2-a]pyridine-8-carbonitrile(cas: 136117-70-9) belongs to imidazoles.Imidazole rings are also present in imidazole ring alkaloids, which are potential therapeutics for thrombosis, cancer and inflammatory diseases.Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《Synthesis of bridgehead nitrogen compounds which contain the benzimidazole moiety. 2,3-Dihydro-1H-pyrrolo[1,2-a]benzimidazoles》 was published in Journal of Heterocyclic Chemistry in 1966. These research results belong to Freedman, Allan R.; Payne, Delbert S.; Day, Allan R.. Recommanded Product: 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol The article mentions the following:

An improved synthetic procedure has been developed for the preparation of the title compounds (I). Of the monosubstituted derivatives, only chloro-2,8-dihydro-1H-pyrrolo[1,2-a]benzimidazole was shown to be a mixture of the 6- and 7-isomers. In the part of experimental materials, we found many familiar compounds, such as 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9Recommanded Product: 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol)

3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9) belongs to imidazoles.Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine. In addition, imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies. Recommanded Product: 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem