Category: pyrimidines

Parmar, Udaysinh’s team published research in Journal of Organic Chemistry in 2021 | CAS: 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.Electric Literature of C4H2Cl2N2

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

Lee, Seungbeom’s team published research in Journal of Medicinal Chemistry in 2020 | 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

《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

Rehberg, Nidja’s team published research in Journal of Medicinal Chemistry in 2020 | 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.Computed Properties of C4H2Cl2N2

《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

Rageot, Denise’s team published research in Journal of Medicinal Chemistry in 2019 | CAS: 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.Reference of 2,4,6-Trichloropyrimidine

The author of 《(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase》 were Rageot, Denise; Bohnacker, Thomas; Keles, Erhan; McPhail, Jacob A.; Hoffmann, Reece M.; Melone, Anna; Borsari, Chiara; Sriramaratnam, Rohitha; Sele, Alexander M.; Beaufils, Florent; Hebeisen, Paul; Fabbro, Doriano; Hillmann, Petra; Burke, John E.; Wymann, Matthias P.. And the article was published in Journal of Medicinal Chemistry in 2019. Reference of 2,4,6-Trichloropyrimidine The author mentioned the following in the article:

The phosphoinositide 3-kinase (PI3K)/mechanistic target of rapamycin (mTOR) pathway is frequently overactivated in cancer, and drives cell growth, proliferation, survival, and metastasis. Here, we report a structure-activity relationship study, which led to the discovery of a drug-like ATP-site PI3K/mTOR kinase inhibitor: (S)-4-(difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530, compound 6), which qualifies as a clin. candidate due to its potency and specificity for PI3K and mTOR kinases, and its pharmacokinetic properties, including brain penetration. Compound 6 showed excellent selectivity over a wide panel of kinases and an excellent selectivity against unrelated receptor enzymes and ion channels. Moreover, compound 6 prevented cell growth in a cancer cell line panel. The preclin. in vivo characterization of compound 6 in an OVCAR-3 xenograft model demonstrated good oral bioavailability, excellent brain penetration, and efficacy. Initial toxicity studies in rats and dogs qualify 6 for further development as a therapeutic agent in oncol. In addition to this study using 2,4,6-Trichloropyrimidine, there are many other studies that have used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Reference of 2,4,6-Trichloropyrimidine) was used in this study.

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.Reference of 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Liang, Xiaofei’s team published research in Journal of Medicinal Chemistry in 2019 | CAS: 1193-21-1

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.Related Products of 1193-21-1

In 2019,Journal of Medicinal Chemistry included an article by Liang, Xiaofei; Wang, Beilei; Chen, Cheng; Wang, Aoli; Hu, Chen; Zou, Fengming; Yu, Kailin; Liu, Qingwang; Li, Feng; Hu, Zhenquan; Lu, Tingting; Wang, Junjie; Wang, Li; Weisberg, Ellen L.; Li, Lili; Xia, Ruixiang; Wang, Wenchao; Ren, Tao; Ge, Jian; Liu, Jing; Liu, Qingsong. Related Products of 1193-21-1. The article was titled 《Discovery of N-(4-(6-acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a potent FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutant selective inhibitor for acute myeloid leukemia》. The information in the text is summarized as follows:

Most of the current FMS-like tyrosine kinase 3 (FLT3) inhibitors lack selectivity between FLT3 kinase and cKIT kinase as well as the FLT3 wt and internal tandem duplication (ITD) mutants. We report a new compound I, which displays GI50 values of 30-80 nM against different ITD mutants and achieves selectivity over both FLT3 wt (8-fold) and cKIT kinase in the transformed BaF3 cells (>300-fold). I potently inhibits the proliferation of the FLT3-ITD-pos. acute myeloid leukemia cancer lines through suppression of the phosphorylation of FLT3 kinase and downstream signaling pathways, induction of apoptosis, and arresting the cell cycle into the G0/G1 phase. I also displays potent antiproliferative effect against FLT3-ITD-pos. patient primary cells, whereas it does not apparently affect FLT3 wt primary cells. In addition, it also exhibits a good therapeutic window to PBMC compared to PKC412. In the in vivo studies, I demonstrates favorable PK profiles and suppresses the tumor growth in the MV4-11 cell inoculated mouse xenograft model. In the experimental materials used by the author, we found 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. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Related Products of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Chukwu, Roxton’s team published research in Organometallics in 1991-07-31 | 3921-01-5

Organometallics published new progress about Crystal structure. 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Category: pyrimidines.

Chukwu, Roxton; Hunter, Allen D.; Santarsiero, Bernard D. published the artcile< Organometallic complexes with electronic bridges. 6. Novel organometallic complexes containing aromatic azines: synthesis and x-ray crystal structure of 4,6-bis[(η5-cyclopentadienyl)dicarbonyliron] 2-(methylthio)pyrimidine>, Category: pyrimidines, the main research area is iron azine complex; pyridine iron complex; pyrazine iron complex; pyridazine iron complex; pyrimidine iron complex; crystal structure iron pyrimidine complex; mol structure iron pyrimidine complex; safety handling mercury.

The syntheses of 13 monometallic and 4 bimetallic complexes in which (η5-C5H5)Fe(CO)2 (Fp; C5H5 = cyclopentadienyl) groups are bound to substituted pyridine, pyrazine, pyridazine, and pyrimidine rings is described. These species are prepared by metathesis reactions between the appropriate number of equivalent of NaFp and the chloro- or fluoro-substituted azine precursors in 25-95% yields and structural factors affecting these yields are discussed. These new materials have been fully characterized by conventional spectroscopic techniques and are shown to contain Fe-C σ-bonds. The x-ray crystal structure of the title complex confirms that it has the expected structure about the pyrimidine ring. It also reveals that, contrary to expectations from frontier MO theory, the (η5-C5H5)Fe(CO)2 groups shows a preference for orientations in which its mirror plane is perpendicular to that of the pyrimidine ring. The spectroscopic data provide no evidence for the existence of any electronic interaction between the metal centers of the new bimetallic azine bridged complexes having meta substitution geometries.

Organometallics published new progress about Crystal structure. 3921-01-5 belongs to class pyrimidines, and the molecular formula is C4H2Br2N2, Category: pyrimidines.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kang, Dongwei’s team published research in Journal of Medicinal Chemistry in 2017-05-25 | 18740-39-1

Journal of Medicinal Chemistry published new progress about Acute toxicity. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Synthetic Route of 18740-39-1.

Kang, Dongwei; Fang, Zengjun; Huang, Boshi; Lu, Xueyi; Zhang, Heng; Xu, Haoran; Huo, Zhipeng; Zhou, Zhongxia; Yu, Zhao; Meng, Qing; Wu, Gaochan; Ding, Xiao; Tian, Ye; Daelemans, Dirk; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong published the artcile< Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants>, Synthetic Route of 18740-39-1, the main research area is thiophene pyrimidine preparation structure based optimization antiviral HIV; HIV antiviral pharmacokinetics cardiotoxicity thiophene pyrimidine.

This work follows on from our initial discovery of a series of piperidine-substituted thiophene[3,2-d]pyrimidine HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTI) (J. Med. Chem. 2016, 59, 7991-8007). In the present study, we designed, synthesized, and biol. tested several series of new derivatives in order to investigate previously unexplored chem. space. Some of the synthesized compounds displayed single-digit nanomolar anti-HIV potencies against wild-type (WT) virus and a panel of NNRTI-resistant mutant viruses in MT-4 cells. I was exceptionally potent against the whole viral panel, affording 3-4-fold enhancement of in vitro antiviral potency against WT, L100I, K103N, Y181C, Y188L, E138K, and K103N+Y181C and 10-fold enhancement against F227L+V106A relative to the reference drug etravirine (ETV) in the same cellular assay. The structure-activity relationships, pharmacokinetics, acute toxicity, and cardiotoxicity were also examined Overall, the results indicate that I is a promising new drug candidate for treatment of HIV-1 infection.

Journal of Medicinal Chemistry published new progress about Acute toxicity. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Synthetic Route of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Rabal, Obdulia’s team published research in ACS Chemical Neuroscience in 2019-09-18 | 89793-12-4

ACS Chemical Neuroscience published new progress about Alzheimer disease. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Related Products of 89793-12-4.

Rabal, Obdulia; Sanchez-Arias, Juan A.; Cuadrado-Tejedor, Mar; de Miguel, Irene; Perez-Gonzalez, Marta; Garcia-Barroso, Carolina; Ugarte, Ana; Estella-Hermoso de Mendoza, Ander; Saez, Elena; Espelosin, Maria; Ursua, Susana; Tan, Haizhong; Wu, Wei; Xu, Musheng; Pineda-Lucena, Antonio; Garcia-Osta, Ana; Oyarzabal, Julen published the artcile< Multitarget Approach for the Treatment of Alzheimer's Disease: Inhibition of Phosphodiesterase 9 (PDE9) and Histone Deacetylases (HDACs) Covering Diverse Selectivity Profiles>, Related Products of 89793-12-4, the main research area is Alzheimer’s disease HDAC inhibition PDE9 inhibition HDAC6 dual inhibitors; Alzheimer’s disease; HDAC6; dual inhibitors; histone deacetylase inhibition; phosphodiesterase 9 inhibition.

Here, we present a series of dual-target phosphodiesterase 9 (PDE9) and histone deacetylase (HDAC) inhibitors devised as pharmacol. tool compounds for assessing the implications of these two targets in Alzheimer’s disease (AD). These novel inhibitors were designed taking into account the key pharmacophoric features of known selective PDE9 inhibitors as well as privileged chem. structures, bearing zinc binding groups (hydroxamic acids and ortho-amino anilides) that hit HDAC targets. These substituents were selected according to rational criteria and previous knowledge from our group to explore diverse HDAC selectivity profiles (pan-HDAC, HDAC6 selective, and class I selective) that were confirmed in biochem. screens. Their functional response in inducing acetylation of histone and tubulin and phosphorylation of cAMP response element binding (CREB) was measured as a requisite for further progression into complete in vitro absorption, distribution, metabolism and excretion (ADME) and in vivo brain penetration profiling. Compound 31b, a selective HDAC6 inhibitor with acceptable brain permeability, was chosen for assessing in vivo efficacy of these first-in-class inhibitors, as well as studying their mode of action (MoA).

ACS Chemical Neuroscience published new progress about Alzheimer disease. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Related Products of 89793-12-4.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reddy, L Srikanth’s team published research in Pharma Innovation in 2018 | 18740-39-1

Pharma Innovation published new progress about Antibacterial agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Quality Control of 18740-39-1.

Reddy, L. Srikanth; Naik, B. Eswar published the artcile< Design, synthesis and characterization of novel thieno[2,3-d]pyrimidines for anti-bacterial and anti-fungal screening>, Quality Control of 18740-39-1, the main research area is thiomorpholinothieno pyrimidine preparation antibacterial antifungal.

A series of novel 4-Substituted and different substituted heterocyclic-N-(2-thiomorpholinothieno[2,3-d]pyrimidin-4-yl)benzamide derivatives I (R = Ph, thiophen-2-yl, 2,5-difluorophenyl, etc.) was synthesized by a facile five-step procedure that afforded advantages of mild reaction conditions, simple protocol and good yields. The final compounds were screened for their antibacterial activity against Staphylococcus aureus (S. aureus) and Bacillus subtilis (B. subtilis) from Gram pos. group of bacteria and Pseudomonas aeruginosa (P. aeruginosa) and Escherichia coli (E. coli) from Gram neg. group of bacteria and antifungal activity against Aspergillus niger (A. niger) and Candida albicans (C. albicans). Anti-bacterial and anti-fungal activities were evaluated and compared with the standard drugs Such as Amoxicillin and Fluconazole from anti-bacterial and antifungal activity screening results, and it has been observed that compounds I (R = thiophen-2-yl, 1-benzothiophen-2-yl, 2,5-difluorophenyl, 4-(trifluoromethyl)phenyl) possess good activity.

Pharma Innovation published new progress about Antibacterial agents. 18740-39-1 belongs to class pyrimidines, and the molecular formula is C6H2Cl2N2S, Quality Control of 18740-39-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jordan, Brian J’s team published research in Polymer Preprints (American Chemical Society, Division of Polymer Chemistry) in 2005-08-31 | 2244-11-3

Polymer Preprints (American Chemical Society, Division of Polymer Chemistry) published new progress about Cyclic voltammetry. 2244-11-3 belongs to class pyrimidines, and the molecular formula is C4H4N2O5, HPLC of Formula: 2244-11-3.

Jordan, Brian J.; Carroll, Joseph B.; Xu, Hao; Erdogan, Belma; Lee, Lisa; Cheng, Lily; Tiernan, Chris; Cooke, Graeme; Rotello, Vincent M. published the artcile< Site isolated redox behavior in flavin functionalized random polystyrene copolymers>, HPLC of Formula: 2244-11-3, the main research area is flavin functionalized random polystyrene copolymer.

A model system has been developed to investigate the individual redox behaviors of flavin derivatives appended onto random polystyrene copolymers through “”click”” chem. procedures. The results indicate that flavin units attached to the polymers exhibit site isolated behavior vs. free flavin, yielding unique fluorescent materials with electrochem. tunable associations upon addition of complementary diamidopyridine functionality.

Polymer Preprints (American Chemical Society, Division of Polymer Chemistry) published new progress about Cyclic voltammetry. 2244-11-3 belongs to class pyrimidines, and the molecular formula is C4H4N2O5, HPLC of Formula: 2244-11-3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia