Category: 3764-01-0

《In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Kang, Dongwei; Feng, Da; Jing, Lanlan; Sun, Yanying; Wei, Fenju; Jiang, Xiangyi; Wu, Gaochan; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong. Related Products of 3764-01-0 The article mentions the following:

HIV-1 RT has been considered as one of the most important targets for the development of anti-HIV-1 drugs for their well-solved three-dimensional structure and well-known mechanism of action. In this study, with HIV-1 RT as target, we used miniaturized parallel click chem. synthesis via CuAAC reaction followed by in situ biol. screening to discover novel potent HIV-1 NNRTIs. A 156 triazole-containing inhibitor library was assembled in microtiter plates and in millimolar scale. The enzyme inhibition screening results showed that 22 compounds exhibited improved inhibitory activity. Anti-HIV-1 activity results demonstrated that A3N19 effected the most potent activity against HIV-1 IIIB (EC50 = 3.28 nM) and mutant strain RES056 (EC50 = 481 nM). The mol. simulation anal. suggested that the hydrogen bonding interactions of A3N19 with the main chain of Lys101 and Lys104 was responsible for its potency. Overall, the results indicated the in situ click chem.-based strategy was rational and might be amenable for the future discovery of more potent HIV-1 NNRTIs.2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products of 3764-01-0) was used in this study.

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Related Products of 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 3764-01-0In 2021 ,《Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies》 appeared in Journal of Medicinal Chemistry. The author of the article were Soares de Melo, Candice; Singh, Vinayak; Myrick, Alissa; Simelane, Sandile B.; Taylor, Dale; Brunschwig, Christel; Lawrence, Nina; Schnappinger, Dirk; Engelhart, Curtis A.; Kumar, Anuradha; Parish, Tanya; Su, Qin; Myers, Timothy G.; Boshoff, Helena I. M.; Barry, Clifton E. III; Sirgel, Frederick A.; van Helden, Paul D.; Buchanan, Kirsteen I.; Bayliss, Tracy; Green, Simon R.; Ray, Peter C.; Wyatt, Paul G.; Basarab, Gregory S.; Eyermann, Charles J.; Chibale, Kelly; Ghorpade, Sandeep R.. The article conveys some information:

Phenotypic screening of a Medicines for Malaria Venture compound library against Mycobacterium tuberculosis (Mtb) identified a cluster of pan-active 2-pyrazolylpyrimidinones. The biol. triage of these actives using various tool strains of Mtb suggested a novel mechanism of action. The compounds were bactericidal against replicating Mtb and retained potency against clin. isolates of Mtb. Although selected MmpL3 mutant strains of Mtb showed resistance to these compounds, there was no shift in the min. inhibitory concentration (MIC) against a mmpL3 hypomorph, suggesting mutations in MmpL3 as a possible resistance mechanism for the compounds but not necessarily as the target. RNA transcriptional profiling and the checkerboard board 2D-MIC assay in the presence of varying concentrations of ferrous salt indicated perturbation of the Fe-homeostasis by the compounds Structure-activity relationship studies identified potent compounds with good physicochem. properties and in vitro microsomal metabolic stability with moderate selectivity over cytotoxicity against mammalian cell lines. After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products of 3764-01-0)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Related Products of 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,European Journal of Organic Chemistry included an article by Bruening, Fabian; Katayev, Dmitry; Togni, Antonio. Synthetic Route of C4HCl3N2. The article was titled 《Facile and Efficient Synthesis of 3-Pyrimidinyl Oxindoles by Phase-Transfer-Catalyzed Regioselective Nucleophilic Aromatic Substitution》. The information in the text is summarized as follows:

Phase-transfer-catalyzed regioselective nucleophilic aromatic substitution of 2,4-dichloropyrimidines with N-Boc-protected 3-substituted oxindoles is reported. The reaction allows the formation of unsym. all- carbon quaternary centers in the benzylic position of heteroaromatic scaffolds and proceeds with high chem. yield and excellent functional-group tolerance. Various activated heteroaryl chlorides including dichloropyridazine and activated chloropyridines can also be reacted under the reaction conditions. The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Synthetic Route of C4HCl3N2)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Synthetic Route of C4HCl3N2

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2017,Bruening, Fabian; Lovelle, Lucie E. published 《Highly regioselective organocatalytic SNAr amination of 2,4-dichloropyrimidine and related heteroaryl chlorides》.European Journal of Organic Chemistry published the findings.Safety of 2,4,6-Trichloropyrimidine The information in the text is summarized as follows:

A highly efficient and regioselective method for the SNAr amination of 2,4-dichloropyrimidine with oxazolidin-2-one and related weakly nucleophilic amines, using sodium sulfinate and tetrabutylammonium bromide as catalysts, is disclosed. This strategy facilitates the synthesis of various aminopyrimidines, e.g., I, in a regio- and chemoselective manner. This approach was successfully used for the amination of various activated N-heteroaromatic substrates. The experimental process involved the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Safety of 2,4,6-Trichloropyrimidine)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Safety of 2,4,6-Trichloropyrimidine

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Redox-Active Reagents for Photocatalytic Generation of the OCF3 Radical and (Hetero)Aryl C-H Trifluoromethoxylation》 was written by Zheng, Weijia; Lee, Johnny W.; Morales-Rivera, Cristian A.; Liu, Peng; Ngai, Ming-Yu. Category: pyrimidinesThis research focused ontrifluoromethoxyarene trifluoromethoxyheteroarene preparation; arene heteroarene radical trifluoromethoxylation ruthenium photocatalyst; arenes; photocatalysis; radicals; trifluoromethoxylating reagents; trifluoromethoxylation. The article conveys some information:

The trifluoromethoxy (OCF3) radical is of great importance in organic chem. Yet, the catalytic and selective generation of this radical at room temperature and pressure remains a longstanding challenge. Herein, the design and development of a redox-active cationic reagent (1) that enables the formation of the OCF3 radical in a controllable, selective, and catalytic fashion under visible-light photocatalytic conditions is reported. More importantly, the reagent allows catalytic, intermol. C-H trifluoromethoxylation of a broad array of (hetero)arenes and biorelevant compounds Exptl. and computational studies suggest single electron transfer (SET) from excited photoredox catalysts to 1 resulting in exclusive liberation of the OCF3 radical. Addition of this radical to (hetero)arenes gives trifluoromethoxylated cyclohexadienyl radicals that are oxidized and deprotonated to afford the products of trifluoromethoxylation. In the experiment, the researchers used many compounds, for example, 2,4,6-Trichloropyrimidine(cas: 3764-01-0Category: pyrimidines)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Category: pyrimidines

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Pyrimidine | C4H4N2 – PubChem,
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Formula: C4HCl3N2In 2017 ,《Sensitization-Initiated Electron Transfer for Photoredox Catalysis》 was published in Angewandte Chemie, International Edition. The article was written by Ghosh, Indrajit; Shaikh, Rizwan S.; Koenig, Burkhard. The article contains the following contents:

Photosynthetic organisms exploit antenna chromophores to absorb light and transfer excitation energy to the reaction center where redox reactions occur. In contrast, in visible-light chem. photoredox catalysis, a single species (i.e., the photoredox catalyst) absorbs light and performs the redox chem. Mimicking the energy flow of the biol. model, we report a two-center photoredox catalytic approach in which the tasks of light energy collection and electron transfer (i.e., redox reactions) are assigned to two different mols. Ru(bpy)3Cl2 absorbs the visible light and transfers the energy to polycyclic aromatic hydrocarbons that enable the redox reactions. This operationally simple sensitization-initiated electron transfer enables the use of arenes that do not absorb visible light, such as anthracene or pyrene, for photoredox applications. We demonstrate the merits of this approach by the reductive activation of chem. bonds with high reduction potentials for carbon-carbon and carbon-heteroatom bond formations. In the experiment, the researchers used many compounds, for example, 2,4,6-Trichloropyrimidine(cas: 3764-01-0Formula: C4HCl3N2)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Formula: C4HCl3N2

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《Novel influenza polymerase PB2 inhibitors for the treatment of influenza A infection》 were Zhang, Hongwang; Zhou, Longhu; Amichai, Sarah; Zandi, Keivan; Cox, Bryan; Schinazi, Raymond; Amblard, Franck. And the article was published in Bioorganic & Medicinal Chemistry Letters in 2019. COA of Formula: C4HCl3N2 The author mentioned the following in the article:

Exploration of the chem. space of known influenza polymerase PB2 inhibitor Pimodivir, was performed by our group. We synthesized and identified compounds I and II, two novel thienopyrimidine derivatives displaying anti-influenza A activity in the single digit nanomolar range in cell culture. Binding of these unique compounds in the influenza polymerase PB2 pocket was also determined using mol. modeling. In the experiment, the researchers used many compounds, for example, 2,4,6-Trichloropyrimidine(cas: 3764-01-0COA of Formula: C4HCl3N2)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.COA of Formula: C4HCl3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2015,Linton, Maria Angelica; Burke, Benjamin J.; Johnson, Ted W.; Ninkovic, Sacha; Gajiwala, Ketan S.; Richardson, Paul; Le, Phuong T. published 《Effect of water solvation on the lipophilicity of isomeric pyrimidine-carboxamides》.Bioorganic & Medicinal Chemistry published the findings.Related Products of 3764-01-0 The information in the text is summarized as follows:

Incorporation of nitrogen is a common medicinal chem. tactic to reduce log D values. Neighboring group participation influences log D, so the results are isomer dependent. The log D and log P differences observed between isomeric pyrimidines 1, 2 and 3 presumably result when the carbonyl or ether lone pairs are in close proximity to a heterocyclic nitrogen lone pair, recruiting water to bridge between the electron rich atoms. Various lipophilicity calculators did not discriminate between 1 (log D = 2.6) and 3 (log D = 1.0), but solvation energies using Poisson-Boltzmann and 3D-RISM methods rationalize the observed differences in lipophilicity among pyrimidine carboxamide isomers. After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products of 3764-01-0)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Related Products of 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2015,Argade, Ankush; Bhamidipati, Somasekhar; Li, Hui; Carroll, David; Clough, Jeffrey; Keim, Holger; Sylvain, Catherine; Rossi, Alexander B.; Coquilla, Christina; Issakani, Sarkiz D.; Masuda, Esteban S.; Payan, Donald G.; Singh, Rajinder published 《Application of cultured human mast cells (CHMC) for the design and structure-activity relationship of IgE-mediated mast cell activation inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Product Details of 3764-01-0 The information in the text is summarized as follows:

Here we report the optimization of small mol. inhibitors of human mast cell degranulation via anti-IgE-mediated tryptase release following crosslinking and activation of IgE-loaded FcεR1 receptors. The compounds are selective upstream inhibitors of FcεR1-dependent human mast cell degranulation and proved to be devoid of activity in downstream ionomycin mediated degranulation. Structure-activity relationship (SAR) leading to compound 26 is outlined. In the experiment, the researchers used many compounds, for example, 2,4,6-Trichloropyrimidine(cas: 3764-01-0Product Details of 3764-01-0)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Product Details of 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Development of a Multikilogram Scale Synthesis of a TRPV1 Antagonist》 was written by Kuethe, Jeffrey T.; Journet, Michel; Peng, Zhihui; Zhao, Dalian; McKeown, Arlene; Humphrey, Guy R.. Reference of 2,4,6-TrichloropyrimidineThis research focused onTRPV1 antagonist preparation. The article conveys some information:

A highly efficient, regioselective five-step synthesis of the TRPV1 antagonist 1 is described. The coupling of piperazine 7 with dichloropyrimidine 8 proceeded via a regioselective Pd-mediated amination affording product 11 in excellent yield. Conversion of the penultimate product 14 afforded 1 through formation of a magnesium ate complex and trapping with CO2. In the part of experimental materials, we found many familiar compounds, such as 2,4,6-Trichloropyrimidine(cas: 3764-01-0Reference of 2,4,6-Trichloropyrimidine)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Reference of 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia