Category: 3934-20-1

《An efficient and scalable approach for the synthesis of piperazine based glitazone and its derivatives》 was published in Synthetic Communications in 2020. These research results belong to Sharma, Vijay Kumar; Barde, Anup; Rattan, Sunita. SDS of cas: 3934-20-1 The article mentions the following:

A versatile and efficient synthetic approach has been developed for the synthesis of piperazine based glitazones I (R = Me, propan-2-yl, cyclopropylmethyl, etc.) analogus to Lobeglitazone. Desired compounds I were synthesized with good yields by alkylation of piperazine substrate I (R = H) with various carbonyl compds R1C(O)R2 (R1 = H, Me, Et, cyclopropyl; R2 = H, Me; R1R2 = -(CH2)3-). This substrate has the potential for the construction of novel heterocyclic compounds with medicinal importance. In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1SDS of cas: 3934-20-1)

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.SDS of cas: 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Raubo, Piotr; Carbajo, Rodrigo J.; McCoull, William; Raubo, Joanna; Thomas, Morgan published an article in 2021. The article was titled 《Diversity-orientated synthesis of macrocyclic heterocycles using a double SNAr approach》, and you may find the article in Organic & Biomolecular Chemistry.Recommanded Product: 3934-20-1 The information in the text is summarized as follows:

An efficient macrocyclization approach based on the double aromatic nucleophilic substitution (SNACK) was developed. This methodol. allows a facile incorporation of heterocyclic motifs into macrocyclic rings and rapid synthesis of a significant number of structurally diverse macrocycles e.g., I. SNACK macrocyclization enables preparation of stable diastereoisomers of conformationally restricted macrocycles (atropisomers) e.g., II and e.g., III. Practical application of SNACK macrocyclization in a drug discovery project was exemplified by the identification of high affinity macrocyclic binders of B-cell lymphoma 6 (BCL6). The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Recommanded Product: 3934-20-1)

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.Recommanded Product: 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Parmar, Udaysinh; Somvanshi, Dipesh; Kori, Santosh; Desai, Aman A.; Dandela, Rambabu; Maity, Dilip K.; Kapdi, Anant R. published an article in 2021. The article was titled 《Room-Temperature Amination of Chloroheteroarenes in Water by a Recyclable Copper(II)-Phosphaadamantanium Sulfonate System》, and you may find the article in Journal of Organic Chemistry.Electric Literature of C4H2Cl2N2 The information in the text is summarized as follows:

The current report discusses about an efficient copper-based catalytic system (Cu/PTABS) for the amination of chloroheteroarenes RCl (R = pyrazinyl, 1,3-benzothiazol-2-yl, 9H-purin-6-yl, etc.) at ambient temperature in water as the sole reaction solvent, a combination that is first to be reported. A wide variety of chloroheteroarenes could be coupled efficiently with primary and secondary amines, e.g., morpholine as well as selected amino acid esters, e.g., L-valine Me ester hydrochloride under mild reaction conditions. Catalytic efficiency of the developed protocol also promotes late-stage functionalization of active pharmaceutical ingredients, e.g., I (APIs) such as antibiotics (floxacins) and anticancer drugs. The catalytic system also performs efficiently at a very low concentration of 0.0001 mol% (TON = 980,000) and can be recycled 12 times without any appreciable loss in activity. Theor. calculations reveal that the π-acceptor ability of the ligand PTABS is the main reason for the appreciably high reactivity of the catalytic system. Preliminary characterization of the catalytic species in the reaction was carried out using UV-VIS and ESR spectroscopy, providing evidence for the Cu(II) oxidation state. In the experiment, the researchers used many compounds, for example, 2,4-Dichloropyrimidine(cas: 3934-20-1Electric Literature of 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.Electric Literature of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Lee, Seungbeom; Kim, Dae Gyu; Kim, Kyeojin; Kim, Taewoo; Lim, Semi; Kong, Hyejin; Kim, Sunghoon; Suh, Young-Ger. SDS of cas: 3934-20-1 The article mentions the following:

Aminoacyl-tRNA synthetase interacting multifunctional proteins (AIMPs) have recently been considered novel therapeutic targets in several cancers. In this publication we report the development of novel 2-aminophenylpyrimidines as new AIMP2-DX2 inhibitors. In particular, aminophenylpyrimidine 3 not only exhibited promising in vitro and in vivo potency but also exerted selective inhibition of H460 and A549 cells and AIMP2-DX2 rather than WI-26 cells and AIMP2. Aminophenylpyrimidine 3 offers possible therapeutic potential in the treatment of lung cancer. In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1SDS of cas: 3934-20-1)

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.SDS of cas: 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial In Vitro and In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Rehberg, Nidja; Sommer, Gereon A.; Driessen, Daniel; Kruppa, Marco; Adeniyi, Emmanuel T.; Chen, Shang; Wang, Lin; Wolf, Karina; Tasch, Boris O. A.; Ioerger, Thomas R.; Zhu, Kui; Mueller, Thomas J. J.; Kalscheuer, Rainer. Computed Properties of C4H2Cl2N2 The article mentions the following:

Natural bisindole alkaloids such as Hyrtinadine A and Alocasin A, which are known to exhibit diverse bioactivities, provide promising chem. scaffolds for drug development. By optimizing the Masuda borylation-Suzuki coupling sequence, a library of various natural product-derived and non-natural (di)azine-bridged bisindoles was created. While unsubstituted bisindoles were devoid of antibacterial activity, 5,5′-chloro derivatives were highly active against methicillin-resistant Staphylococcus aureus (MRSA) and further Gram-pos. pathogens at minimal inhibitory concentrations ranging from 0.20 to 0.78μM. These compounds showed strong bactericidal killing effects but only moderate cytotoxicity against human cell lines. Furthermore, the two front-runner compounds 4j and 4n exhibited potent in vivo efficacy against MRSA in a mouse wound infection model. Although structurally related bisindoles were reported to specifically target pyruvate kinase in MRSA, antibacterial activity of 4j and 4n is independent of pyruvate kinase. Rather, these compounds lead to bacterial membrane permeabilization and cellular efflux of low-mol.-weight mols. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Computed Properties of C4H2Cl2N2)

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.Computed Properties of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of 2,4-DichloropyrimidineIn 2021 ,《Discovery of N-(4-(3-isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-4-(4-methylpiperazin-1-yl)quinazolin-7-amine as a Novel, Potent, and Oral Cyclin-Dependent Kinase Inhibitor against Haematological Malignancies》 was published in Journal of Medicinal Chemistry. The article was written by Huang, Jianhang; Wang, Xinren; Dong, Ruinan; Liu, Xiaoyue; Li, Hongmei; Zhang, Tianyi; Xu, Junyu; Liu, Chenhe; Zhang, Yanmin; Hou, Shaohua; Tang, Weifang; Lu, Tao; Chen, Yadong. The article contains the following contents:

Hematol. malignancies (HM) start in blood forming tissue or in the cells of the immune system. Cyclin-dependent kinases (CDKs) regulate cell cycle progression, and some of them control cellular transcription. CDK inhibition can trigger apoptosis and could be particularly useful in hematol. malignancies. Herein, we describe our efforts toward the discovery of a novel series of quinazoline derivatives as CDK inhibitors. Intensive structural modifications lead to the identification of compound 37d as the most active inhibitors of CDKs 1, 2, 4, 8 and 9 with balancing potency and selectivity against CDKs. Further biol. studies revealed that compound 37d can arrest the cell cycle and induce apoptosis via activating PARP and caspase 3. More importantly, compound 37d showed good antitumor efficacy in multiple HM mice xenograft models with no obvious toxicity. These results indicated that CDK 1, 2, 4, 8, and 9 inhibitors could be potentially used to treat certain hematol. malignancies. In the experiment, the researchers used 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 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 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

COA of Formula: C4H2Cl2N2In 2019 ,《Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of non-small cell lung cancer》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Wang, Xueyuan; Bai, Enhe; Zhou, Hui; Sha, Sijia; Miao, Hang; Qin, Yanru; Liu, Zhaogang; Wang, Jia; Zhang, Haoyang; Lei, Meng; Liu, Jia; Hai, Ou; Zhu, Yongqiang. The article conveys some information:

Valosine containing protein (VCP/p97) is a member of the AAA ATPase family involved in several essential cellular functions and plays an important role in the ubiquitin-mediated degradation of misfolded proteins. P97 has a significant role in maintaining the cellular protein homeostasis for tumor cell growth and survival and has been found overexpressed in many tumor types. No new mol. entities based on p97 target were approved in clinic. Herein, a series of novel pyrimidine structures as p97 inhibitors were designed and synthesized. After enzymic evaluations, structure-activity relationships (SAR) were discussed in detailed. Among the screened compounds, derivative 35 showed excellent enzymic inhibitory activity (IC50, 36 nM). The cellular inhibition results showed that compound 35 had good antiproliferative activity against the non-small cell lung cancer A549 cells (IC50, 1.61 μM). Liver microsome stability showed that the half-life of compound 35 in human liver microsome was 42.3 min, which was more stable than the control CB-5083 (25.8 min). The in vivo pharmacokinetic results showed that the elimination phase half-lives of compound 35 were 4.57 h for ig and 3.64 h for iv, resp. and the oral bioavailability was only 4.5%. These results indicated that compound 35 could be effective for i.v. treatment of non-small cell lung cancer. In the experiment, the researchers used many compounds, for example, 2,4-Dichloropyrimidine(cas: 3934-20-1COA of Formula: C4H2Cl2N2)

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Meng, Fan-Jie; Shao, Bing-Ru; Velopolcek, Maria K.; Guo, Xuan; Feng, Guang-Shou; Shi, Lei published their research in Organic & Biomolecular Chemistry in 2021. The article was titled 《Redox deracemization of phosphonate-substituted dihydropyrimidines》.Name: 2,4-Dichloropyrimidine The article contains the following contents:

An efficient redox deracemization of the phosphonic ester substituted 3,4-dihydropyrimidin-2-one (DHPM) derivatives I (R = Ph, Me, naphth-2-yl, etc.; R1 = H, Me, Ph) is described. The one-pot deracemization strategy consisted of the oxidization to destroy the stereocenter center and the following asym. transfer hydrogenation to regenerate the chiral carbon center with the vicinal phosphonic ester group, providing a series of optically active phosphonate substituted DHPMs with up to 96% ee. The results came from multiple reactions, including the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Name: 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.Name: 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Computed Properties of C4H2Cl2N2In 2020 ,《Discovery of novel 2,4-disubstituted pyrimidines as Aurora kinase inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Xu, Yu; Hao, Shu-Yi; Zhang, Xiu-Juan; Li, Wen-Bo; Qiao, Xue-Peng; Wang, Zi-Xiao; Chen, Shi-Wu. The article conveys some information:

In order to explore novel Aurora kinase inhibitors, a series of novel 2,4-disubstituted pyrimidines were designed, synthesized and evaluated their in vitro anti-proliferative activities against a panel of cancerous cell lines (A549, HCT-116 and MCF-7). Among them, compound 12a (I) showed moderate to high anti-proliferative activities against A549 (IC50 = 12.05 ± 0.45μM), HCT-116 (IC50 = 1.31 ± 0.41μM) and MCF-7 (IC50 = 20.53 ± 6.13μM) cells, as well as the Aurora A and Aurora B inhibitory activities with the IC50 values of 309 nM and 293 nM, resp. Furthermore, compound 12a induced apoptosis by upregulating the pro-apoptotic proteins Bax and decreased the anti-apoptotic protein Bcl-xl in HCT-116 cells. Moreover, the mol. docking study showed that compound 12a had good binding modes with Aurora A and Aurora B and the bioinformatics prediction discovered that compound 12a exhibited good drug likeness using SwissADME. Taken together, these results indicated that 12a may be a potential anticancer compound that was worthy of further development as Aurora kinase inhibitor. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Computed Properties of C4H2Cl2N2)

2,4-Dichloropyrimidine(cas: 3934-20-1) 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.Computed Properties of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Drewry, David H.; Annor-Gyamfi, Joel K.; Wells, Carrow I.; Pickett, Julie E.; Dederer, Verena; Preuss, Franziska; Mathea, Sebastian; Axtman, Alison D. published an article in Journal of Medicinal Chemistry. The title of the article was 《Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration》.Quality Control of 2,4-Dichloropyrimidine The author mentioned the following in the article:

The pyrimidine core has been utilized extensively to construct kinase inhibitors, including eight FDA-approved drugs. Because the pyrimidine hinge-binding motif is accommodated by many human kinases, kinome-wide selectivity of resultant mols. can be poor. This liability was seen as an advantage since it is well tolerated by many understudied kinases. We hypothesized that nonexemplified aminopyrimidines bearing side chains from well-annotated pyrimidine-based inhibitors with off-target activity on understudied kinases would provide us with useful inhibitors of these lesser studied kinases. Our strategy paired mixing and matching the side chains from the 2- and 4-positions of the parent compounds with modifications at the 5-position of the pyrimidine core, which is situated near the gatekeeper residue of the binding pocket. Utilizing this approach, we imparted improved kinome-wide selectivity to most members of the resultant library. Importantly, we also identified potent biochem. and cell-active lead compounds for understudied kinases like DRAK1, BMP2K, and MARK3/4. In the experiment, the researchers used many compounds, for example, 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. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Quality Control of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia