Pyrimidines

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

Manzoor, Shoaib; Petreni, Andrea; Raza, Kausar Md; Supuran, Claudiu T.; Hoda, Nasimul published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies》.Quality Control of 2,4-Dichloropyrimidine The article contains the following contents:

A series of new triazole-sulfonamide bearing pyrimidine derivatives I [R = H, Me; R1 = morpholino, 4-methylpiperazin-1-yl, 4-(4-methoxyphenyl)piperazin-1-yl, etc.] were designed and synthesized via click chem. All new compounds I were validated by 1HNMR, 13CNMR, HRMS and compound I [R = H, R1 = 1-piperidyl] was further structurally validated by X-Ray single diffraction study. These compounds I were tested as inhibitors of human carbonic anhydrase (hCA) isoforms, such as hCA I, II, IX and XII, using a stopped flow CO2 hydrase assay. Most of the compounds exhibited significant inhibitory activity against hCA II and weak inhibitory activity against hCA I. The target compounds also displayed moderate to excellent inhibitory activity against tumor-related hCAs IX and XII. Some compounds, e.g., I [R = Me, R1 = 4-(4-methoxyphenyl)piperazin-1-yl, 4-ethoxycarbonylpiperazin-1-yl, 4-(2-methoxyphenyl)piperazin-1-yl] with Ki = 9.4 nM, 1.8 nM, 0.82 nM resp. exhibited excellent inhibitory activity and selectivity profile against hCAs XII over IX. Compound I [R = Me, R1 = 4-(4-chlorobenzyl)piperazin-1-yl] displayed promising inhibitory activity and selectivity profile against both tumor-related hCAs IX (Ki = 2.9 nM) as well as XII (Ki = 0.82 nM) over hCA I and II. To understand the mol. interactions, mol. docking study of compounds I [R = Me, R1 = 4-methoxyphenyl, 4-(4-chlorobenzyl)piperazin-1-yl, 4-ethoxycarbonylpiperazin-1-yl, 4-(2-methoxyphenyl)piperazin-1-yl] with hCA XII and I [R = Me, R1 = 4-(4-chlorobenzyl)piperazin-1-yl] also with hCA IX were performed. The computational study evidenced favorable interaction between the inhibitors and active residues of both proteins. Some of these derivatives are promising leads for the development of selective, anticancer agents based on CA inhibitors. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloropyrimidine(cas: 3934-20-1Quality Control of 2,4-Dichloropyrimidine)

2,4-Dichloropyrimidine(cas: 3934-20-1) 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.Quality Control of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Maimaitiyiming, Xieraili; Shi, Caijin published their research in Materials Chemistry and Physics in 2021. The article was titled 《Poly(1,4-diethynylphenylene-4,6-pyrimidine)s for fluorescence detection of mercury(II) ion》.Category: pyrimidines The article contains the following contents:

A series of alternating conjugated polymers (poly (1,4-diethynylphenylene-4,6-pyrimidine) (PI) and poly (2,5-diheptyloxy-1,4-diethynyl-phenylene-4,6-pyrimidine) (PII) were synthesized via Sonogashira coupled reaction. Chem. structure of conjugated polymers were certified by NMR and FT-IR. The PIII(poly(2,5-bis(dodecoxy)-1,4-diethynyl-phenylene-4,6-pyrimidine) previously reported by our group to illustrate the application of such polymer. The fluorescence of PIII were efficiently quenched when introduced I-, the specificity of the polymer for I- was verified by experiments and detection limit reaches 5.19 x 10-7 mol/L. Thanks to the high association constant between Hg2+ and I-, the fluorescence of PIII/I- system recovered with the addition of Hg2+. The detection limit of Hg2+ reaches ∼4.92 x 10-6 mol/L for PIII/I- complex system. PIII/I- could act as high selective, sensitive and anti-interference optical probe for Hg2+. In the part of experimental materials, we found many familiar compounds, such as 4,6-Dichloropyrimidine(cas: 1193-21-1Category: pyrimidines)

4,6-Dichloropyrimidine(cas: 1193-21-1) 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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Polyionic gels: efficient heterogeneous media for metal scavenging and catalysis》 was written by Thiot, Carine; Schmutz, Marc; Wagner, Alain; Mioskowski, Charles. Category: pyrimidines And the article was included in Angewandte Chemie, International Edition on April 28 ,2006. The article conveys some information:

A highly polar micro-environment, which is suitable for efficient metal scavenging and heterogeneous catalyst preparation, is provided by polyionic gel beads prepared from chloromethylated polystyrene (Merrifield resin) and triethylamine or trioctylamine. Complexation of palladium acetate by resin-bound ammonium salts with or without anion exchange provides effective resin-bound recyclable palladium ionic gel catalysts for Suzuki coupling reactions of aryl and heteroaryl bromides with aryl and heteroaryl boronic acids to give biaryls. The heterogeneous media enable easy product isolation and catalyst recycling. The resin-bound benzyltriethylammonium chloride-supported palladium catalyst forms gel-embedded palladium colloid particles under Suzuki coupling reaction conditions. Phenylacetylene is regioselectively and stereoselectively hydrosilylated with diethoxymethylsilane in the presence of a complex derived from the resin-bound benzyltriethylammonium chloride and Wilkinson’s catalyst to give (E)-PhC:CHSiMe(OEt)2 in 89% yield. In addition to this study using 3-(Pyrimidin-5-yl)benzaldehyde, there are many other studies that have used 3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6Category: pyrimidines) was used in this study.

3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Ylides of heterocycles. VII. Iodonium-, nitrogen-, phosphonium-, and sulfonium-ylides of pyrimidones》 was written by Habib, Nargues Samuel; Kappe, Samuel. SDS of cas: 15726-38-2 And the article was included in Journal of Heterocyclic Chemistry on April 30 ,1984. The article conveys some information:

Reaction of pyrimidinone I (R = OH; R1 = H, Me, Ph, R2 = H; R1 = R2 = Ph; R3 = H) with PhIO prepared in situ gave iodonium ylides I (R = O-, R3 = PhI+; II) in good yield. Thermal rearrangement of II gave I (R = OPh; R3 = iodo), which were deiodinated to give I (R = OPh, R3 = H). Treatment of II with pyridine, nicotinamide, isoquinoline, Ph3P, or thiophene gave the corresponding N, P, or S ylides. The pyridinium ylides were also prepared from I (R = OH, R1 = Br, Cl) which were prepared from II by treatment with HBr or HCl, resp. In the experiment, the researchers used 5-Bromo-4,6-dihydroxypyrimidine(cas: 15726-38-2SDS of cas: 15726-38-2)

5-Bromo-4,6-dihydroxypyrimidine(cas: 15726-38-2) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.SDS of cas: 15726-38-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

HPLC of Formula: 122567-97-9On March 31, 1994, Tortolani, David R.; Russell, John W.; Whiterock, Valerie J.; Hitchcock, Michael J. M.; Ghazzouli, Ismail; Martin, John C.; Mansuri, Muzammil M.; Starrett, John E. Jr. published an article in Journal of Pharmaceutical Sciences. The article was 《Prodrugs of 2′,3′-Didehydro-3′-deoxythymidine (D4T): Synthesis, Antiviral Activity, and Rapid Pharmacokinetic Evaluation》. The article mentions the following:

A series of 5′-derivatives and modified pyrimidine analogs of 2′,3′-didehydro-3′-deoxythymidine (d4T, stavudine) were synthesized to determine their potential as oral prodrugs of d4T. Utilizing a screen developed for the rapid evaluation of a variety of prodrugs in mice, it was determined that 5′-acetate provided comparable plasma levels of d4T after oral administration of the prodrug to that when d4T was administered alone. The relative oral bioavailability of methoxy acetate and cyclohexyl carbonate derivatives was 79 and 41%, resp. The dihydropyridine ester did not provide detectable levels of d4T up to 1 h after oral administration of 6. Thiopyrimidine and aminopyrimidine derivatives also failed to provide measurable levels of d4T after oral administration. 5′-Derivatives showed similar activity to that of d4T against HIV and MuLV, as did 5′-benzoyl-4-thio derivative However, the corresponding 4-thio 5′-alc. derivative was inactive. In the experimental materials used by the author, we found ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9HPLC of Formula: 122567-97-9)

((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.HPLC of Formula: 122567-97-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 213743-31-8On October 2, 2000 ,《Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Arnold, L. D.; Calderwood, D. J.; Dixon, R. W.; Johnston, D. N.; Kamens, J. S.; Munschauer, R.; Rafferty, P.; Ratnofsky, S. E.. The article contains the following contents:

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of lck in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Application of 213743-31-8)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Application of 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylateOn October 8, 2009 ,《RNase H Active Site Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase: Design, Biochemical Activity, and Structural Information》 was published in Journal of Medicinal Chemistry. The article was written by Kirschberg, Thorsten A.; Balakrishnan, Mini; Squires, Neil H.; Barnes, Tiffany; Brendza, Katherine M.; Chen, Xiaowu; Eisenberg, Eugene J.; Jin, Weili; Kutty, Nilima; Leavitt, Stephanie; Liclican, Albert; Liu, Qi; Liu, Xiaohong; Mak, John; Perry, Jason K.; Wang, Michael; Watkins, William J.; Lansdon, Eric B.. The article contains the following contents:

Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These mols. can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymic activity was measured in a biochem. assay, but no antiviral effect was observed Binding was demonstrated via a solid state structure of the isolated p15-Ec domain of HIV-1 RT showing inhibitor and two Mn(II) ions bound to the RNase H active site. The experimental part of the paper was very detailed, including the reaction process of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6Application In Synthesis of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate)

Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Application In Synthesis of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylateThey have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Category: pyrimidinesOn September 18, 2020 ,《Development of a Scalable Route for a Highly Polar Heterocyclic Aminocyclopropyl Building Block》 was published in Organic Process Research & Development. The article was written by Schafer, Gabriel; Ahmetovic, Muhamed; Fleischer, Tony; Abele, Stefan. The article contains the following contents:

A robust and scalable route toward key heterocyclic building block 1-(pyrimidin-2-yl)cyclopropan-1-amine hydrochloride from cyclopropanated starting material 1-amino-1-cyclopropanecarbonitrile hydrochloride was successfully developed. The key to success was the construction of a pyrimidine ring via cyclization from an amidine intermediate and a bench-stable 2-chloro vinamidinium hexafluorophosphate salt. The cyclization was performed under mild conditions, and the resulting 4-chloropyrimidine derivative was isolated in high yield and purity. The final hydrogenation was intensively optimized: A combination of Pd(OH)2/C as a catalyst and NaOMe as a base at 1 bar H2 pressure in MeOH simultaneously cleaved the Cbz group and dechlorinated the pyrimidine ring while at the same time suppressing the over-reduction of the pyrimidine ring to below 1.0%. After acidification with HCl, followed by removal of the catalyst and NaCl by filtration, the final product was isolated in high yield and purity as a bench-stable off-white solid. The overall yield of the five-step sequence was 57%. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3Category: pyrimidines)

Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia