Day: October 20, 2022

《Human spleen dihydroorotate dehydrogenase: a study of inhibition of the enzyme》 was written by Gero, Annette M.; O’Sullivan, William J.; Brown, Desmond. Related Products of 15726-38-2 And the article was included in Biochemical Medicine on August 31 ,1985. The article conveys some information:

Numerous pyrimidine analogs were tested as possible inhibitors of human spleen mitochondrial dihydroorotate dehydrogenase (DHO DHase). Of these, 9 were demonstrated to be effective inhibitors of the enzymic activity. Two compounds, dihydro-5-azaorotate and 6-thiobarbiturate, appeared to be specific inhibitors of the DHO DHase. In addition, 3 compounds, 5-azaorotate, 5-bromoorotate, and barbiturate were also inhibitory against the 2 subsequent enzymes of the pathway, orotate phosphoribosyltransferase and orotidylate decarboxylase, so that they could act against 3 enzymes of the mammalian pyrimidine de novo biosynthetic pathway. In the experiment, the researchers used many compounds, for example, 5-Bromo-4,6-dihydroxypyrimidine(cas: 15726-38-2Related Products of 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.Related Products of 15726-38-2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Synthesis and evaluation of antibacterial activity of some new N,N’-(5-(6-(4-substitutedphenyl)imidazo[2,1-b][1,3,4]-thiadiazol-2-yl)pyrimidine-2,4-diyl)diacetamide derivatives》 was published in Pharma Chemica in 2010. These research results belong to Sankangoud, Ramappa M.; Chatni, Nandini B.; Goudanavar, Prakash S.. Reference of Ethyl 2,4-diaminopyrimidine-5-carboxylate The article mentions the following:

A series of new N,N’-(5-(6-(4-substitutedphenyl)imidazo[2,1-b][1,3,4]-thiadiazol-2-yl)pyrimidine-2,4-diyl)diacetamide derivatives, e. g. I, were synthesized and tested for their antibacterial activity. Guanidine carbonate & Et (ethoxymethylene) cyanoacetate were used as the starting materials for the preparation of ethyl-2,4-diaminopyrimidine-5-carboxylate. The reactive amino groups were acetylated using acetic anhydride in presence of DMF to form Et 2,4-diacetamidopyrimidine-5-carboxylate. Efforts without masking the reactive amino groups on pyrimidine at this stage did not yield the target compounds Further Et group from position 5 was removed as ethanol by refluxing with 10% alc. NaOH for 10 min to form 2,4-diacetamidopyrimidine-5-carboxylic acid. This acid was refluxed for 4 h with thiosemicarbazide and phosphorous oxychloride to get N,N’-(5-(5-amino-1,3,4-thiadiazol-2-yl)pyrimidine-2,4-diyl)diacetamide. Further target compounds were synthesized using different substituted phenacyl bromides and their structureswere confirmed by IR and 1H NMR spectroscopy. They were tested for their antibacterial activities using cup-plate-agar-diffusion method and 3 compounds have shown potent activity against both gram-pos. and gram-neg. microorganisms as compared to the standard drug methotrexate. In the experimental materials used by the author, we found Ethyl 2,4-diaminopyrimidine-5-carboxylate(cas: 15400-54-1Reference of Ethyl 2,4-diaminopyrimidine-5-carboxylate)

Ethyl 2,4-diaminopyrimidine-5-carboxylate(cas: 15400-54-1) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Reference of Ethyl 2,4-diaminopyrimidine-5-carboxylate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Computed Properties of C23H22N4OOn March 31, 2010, Marcotte, Douglas J.; Liu, Yu-Ting; Arduini, Robert M.; Hession, Catherine A.; Miatkowski, Konrad; Wildes, Craig P.; Cullen, Patrick F.; Hong, Victor; Hopkins, Brian T.; Mertsching, Elisabeth; Jenkins, Tracy J.; Romanowski, Michael J.; Baker, Darren P.; Silvian, Laura F. published an article in Protein Science. The article was 《Structures of human Bruton’s tyrosine kinase in active and inactive conformations suggest a mechanism of activation for TEC family kinases》. The article mentions the following:

Bruton’s tyrosine kinase (BTK), a member of the TEC family of kinases, plays a crucial role in B-cell maturation and mast cell activation. Although the structures of the unphosphorylated mouse BTK kinase domain and the unphosphorylated and phosphorylated kinase domains of human ITK are known, understanding the kinase selectivity profiles of BTK inhibitors has been hampered by the lack of availability of a high resolution, ligand-bound BTK structure. Here, we report the crystal structures of the human BTK kinase domain bound to either Dasatinib (BMS-354825) at 1.9 Å resolution or to 4-amino-5-(4-phenoxyphenyl)-7H-pyrrolospyrimidin-7-yl-cyclopentane at 1.6 Å resolution This data provides information relevant to the development of small mol. inhibitors targeting BTK and the TEC family of nonreceptor tyrosine kinases. Anal. of the structural differences between the TEC and Src families of kinases near the Trp-Glu-Ile motif in the N-terminal region of the kinase domain suggests a mechanism of regulation of the TEC family members. In the experimental materials used by the author, we found 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Computed Properties of C23H22N4O)

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. Computed Properties of C23H22N4O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of 4,6-Dichloropyrimidin-2(1H)-oneOn June 14, 1989, Huebsch, Walter; Pfleiderer, Wolfgang published an article in Helvetica Chimica Acta. The article was 《Pteridines. Part XLI. Synthesis and properties of 6,7,8-trimethyl-4-thiolumazine》. The article mentions the following:

The first representative I of the 8-substituted 4-thiolumazine series has been synthesized. 4,6-Dichloropyrimidin-2(1H)-one was converted into 4-chloro-6-(methylamino)pyrimidin-2(1H)-one, then the Cl atom was displaced by the thioxo group followed by a coupling reaction with ClC6H4N2+Cl- to introduce the necessary N-function into the 5-position. Reduction of the p-chlorophenylazo group leads to 6-(methylamino)-4-thiouracil-5-amine which on condensation with diacetyl gives I. The phys. properties of I are compared with the 2-thio analog and with 6,7,8-trimethyllumazine indicating that I possesses the highest acidity and the longest UV absorption. The experimental process involved the reaction of 4,6-Dichloropyrimidin-2(1H)-one(cas: 6297-80-9Application In Synthesis of 4,6-Dichloropyrimidin-2(1H)-one)

4,6-Dichloropyrimidin-2(1H)-one(cas: 6297-80-9) 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.Application In Synthesis of 4,6-Dichloropyrimidin-2(1H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2017,Organic Chemistry Frontiers included an article by Liu, Yuan; Yu, Yang; Fu, Yiwei; Liu, Yonghai; Shi, Lei; Li, Hao; Wang, Wei. Computed Properties of C8H10N2O2. The article was titled 《Transition-metal-free synthesis of indolizines via [3 + 2]-annulation from α-bromoenals and 2-substituted azaarenes》. The information in the text is summarized as follows:

A transition-metal-free synthetic approach to synthesize indolizines from α-bromo-substituted enals and simple 2-substituted azaarenes were developed. A variety of functional groups were tolerated under mild reaction conditions. Moreover, Michael addition, intramol. N-alkylation and aromatization were involved in this convergent and feasible “”one-pot”” tandem reaction to afford the annulation products in moderate to good yields. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3Computed Properties of C8H10N2O2)

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.Computed Properties of C8H10N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2019,Polymers (Basel, Switzerland) included an article by Dong, Xue; Xing, Tieling; Chen, Guoqiang. Recommanded Product: 2,4,6-Trichloropyrimidine. The article was titled 《Durable antipilling modification of cotton fabric with chloropyrimidine compounds》. The information in the text is summarized as follows:

Cotton fabric, a natural cellulose material, is widely used in the textile industry for its excellent properties. However, its application in some fields are seriously restricted because of its poor antipilling behavior. In this study, cotton fabrics were modified with 2,4,6-trichloropyrimidine (TLP), 2,4-dichloro-5-methoxypyrimidine (DMP), and 2-amino-4,6-dichloropyridine (ADP). The surface morphol. and chem. structure of the modified cotton fabric were characterized by SEM, Fourier transform IR spectroscopy (FTIR), and X-ray diffraction (XRD). Furthermore, the antipilling behavior, dyeing properties, thermal properties, and mech. properties of modified cotton fabric were evaluated. The results showed that chloropyrimidine compounds were successfully grafted onto the surface of the cotton fabric, leading to excellent and durable antipilling activity of grade 3-4 even after 10 washes. Moreover, compared with control cotton fabric, the heat release rate (HRR) and total heat release (THR) of TLP-modified cotton fabric decreased to 173.2 W/g (42.3% reduction) and 11.3 KJ/g (13.7% reduction), resp. In addition, the increased K/S value of modified cotton fabrics dyed with reactive dyes indicated that the modification can enhance the dyability of cotton fabric. This technique provides a simple and versatile method for improving the antipilling behavior of cellulosic materials and supports further preparation of functional textiles. In the experiment, the researchers used many compounds, for example, 2,4,6-Trichloropyrimidine(cas: 3764-01-0Recommanded Product: 2,4,6-Trichloropyrimidine)

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.Recommanded Product: 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Synthesis, Photophysical Properties, and Biological Profiling of Benzothieno-Fused 7-Deazapurine Ribonucleosides》 was written by Yang, Chao; Pohl, Radek; Tichy, Michal; Gurska, Sona; Pavlis, Petr; Dzubak, Petr; Hajduch, Marian; Hocek, Michal. Related Products of 1193-21-1 And the article was included in Journal of Organic Chemistry in 2020. The article conveys some information:

Two isomeric series of benzothieno-fused 7-deazapurine (benzo[4′,5′]thieno[3′,2′:4,5]- and benzo[4′,5′]thieno[2′,3′:4,5]pyrrolo[2,3-d]pyrimidine) ribonucleosides were designed and synthesized. Key steps of the synthesis included the Negishi coupling of zincated dichloropyrimidine with 2- or 3-iodobenzothiophene followed by azidation, thermal or photochem. cyclization, glycosylation, and final functionalization at position 6 through cross-couplings or nucleophilic substitutions. Deprotection gave the final nucleosides, some of which showed moderate cytotoxic and antiviral activity. Most of the free nucleosides showed moderate to strong fluorescence with emission maxima of 362-554 nm. 2′-Deoxyribonucleoside and its 5′-O-triphosphate were also prepared from benzothieno-fused 7-deazaadenine derivative, and the triphosphate was a good substrate for KOD XL DNA polymerase in primer extension synthesis of modified DNA which exerted a weak fluorescence which was slightly enhanced in double-stranded DNA as compared to single-stranded oligonucleotides. The results came from multiple reactions, including the reaction of 4,6-Dichloropyrimidine(cas: 1193-21-1Related Products of 1193-21-1)

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ding, Li; Pannecouque, Christophe; De Clercq, Erik; Zhuang, Chunlin; Chen, Fen-Er published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from N-Alkylation to Methyl Hopping on the Pyrimidine Ring》.Application In Synthesis of 2,4-Dichloropyrimidine The article contains the following contents:

Considering the nonideal metabolic stability of the difluoro-biphenyl-diarylpyrimidine lead compound I, a series of novel alkylated difluoro-biphenyl-diarylpyrimidines were designed and synthesized based on their structure. Introducing alkyl or substituted alkyl groups on the linker region to block the potential metabolic sensitive sites generated 22 derivatives Among them, compound II with an N-Me group displayed excellent anti-HIV-1 activity and selectivity. The Me group was hopped to the central pyrimidine to occupy the small linker region and maintain the water-mediated hydrogen bond observed in the binding of compound I with RT. The resulting compound III exhibited an improved anti-HIV-1 activity, much lower cytotoxicity, and nanomolar activity toward multiple mutants. In addition, III has a better stability in human liver microsomes than I. Moreover, no apparent in vivo acute toxicity was observed in III-treated female, especially pregnant mice. This series of alkylated compounds with highly potency and safety represent a promising lead template for future discovery. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Application In Synthesis of 2,4-Dichloropyrimidine)

2,4-Dichloropyrimidine(cas: 3934-20-1) 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.Application In Synthesis of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Luo, Zaoli; Liu, Yungen; Tong, Ka-Chung; Chang, Xiao-Yong; To, Wai-Pong; Che, Chi-Ming published an article in 2021. The article was titled 《Luminescent Platinum(II) Complexes with Bidentate Diacetylide Ligands: Structures, Photophysical Properties and Application Studies》, and you may find the article in Chemistry – An Asian Journal.Formula: C4H2Cl2N2 The information in the text is summarized as follows:

A series of platinum(II) m-terphenyl 2,2”-diacetylide complexes supported by diimines (2,2′-bipyridines, 1,10-phenanthroline, 2,2′-bipyrimidine) or bis-N-heterocyclic carbenes 3-RIm(CH2)nImR-3′ (R = Bu, Me; n = 1-3) ligands have been prepared The diacetylide ligands adopt a cis coordination mode featuring non-planar terphenyl moieties as revealed by X-ray crystallog. analyses. The electrochem., photophys. and photochem. properties of these platinum(II) complexes have been investigated. These platinum(II) diimine complexes show broad emission with peak maxima from 566 nm to 706 nm, with two of them having emission quantum yields >60% and lifetimes <2μs in solutions at room temperature, whereas the platinum(II) diacetylide complexes having bis-N-heterocyclic carbene instead of diimine ligand display photoluminescence with quantum yields of up to 28% in solutions and excited state lifetimes of up to 62μs at room temperature Application studies revealed that one of the complexes can catalyze photoinduced aerobic dehydrogenation of alcs. and alkenes, and a relatively non-toxic water-soluble Pt(II) complex displays anti-angiogenic activity. After reading the article, we found that the author used 2,4-Dichloropyrimidine(cas: 3934-20-1Formula: C4H2Cl2N2)

2,4-Dichloropyrimidine(cas: 3934-20-1) 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.Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Song, Peilu; Zhao, Fan; Li, Dahong; Qu, Jiqiang; Yao, Miao; Su, Yuan; Wang, Hanxun; Zhou, Miaomiao; Wang, Yujie; Gao, Yinli; Li, Feng; Zhao, Dongmei; Zhang, Fengjiao; Rao, Yu; Xia, Mingyu; Li, Haitao; Wang, Jian; Cheng, Maosheng published an article in Acta Pharmaceutica Sinica B. The title of the article was 《Synthesis of selective PAK4 inhibitors for lung metastasis of lung cancer and melanoma cells》.Reference of 2,4-Dichloropyrimidine The author mentioned the following in the article:

The p21 activated kinase 4 (PAK4) is serine/threonine protein kinase that is critical for cancer progression. Guided by X-ray crystallog. and structure-based optimization, we report a novel subseries of C-3-substituted 6-ethynyl-1H-indole derivatives that display high potential and specificity towards group II PAKs. Among these inhibitors, compound 55 exhibited excellent inhibitory activity and kinase selectivity, displayed superior anti-migratory and anti-invasive properties against the lung cancer cell line A549 and the melanoma cell line B16. Compound 55 exhibited potent in vivo antitumor metastatic efficacy, with over 80% and 90% inhibition of lung metastasis in A549 or B16-BL6 lung metastasis models, resp. Further mechanistic studies demonstrated that compound 55 mitigated TGF-β1-induced epithelial-mesenchymal transition (EMT). In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1Reference of 2,4-Dichloropyrimidine)

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia