Tag: 100-200

Wang, Xiao-Jun; Xu, Yibo; Zhang, Li; Krishnamurthy, Dhileepkumar; Senanayake, Chris H. published an article in Organic Letters. The title of the article was 《Mild Iodine-Magnesium Exchange of Iodoaromatics Bearing a Pyrimidine Ring with Isopropylmagnesium Chloride》.Reference of 3-(Pyrimidin-5-yl)benzaldehyde The author mentioned the following in the article:

(Iodo)arenes bearing a reactive pyrimidine ring underwent a clean iodine-magnesium exchange with isopropylmagnesium chloride in the presence of bis[2-(dimethylamino)ethyl] ether to provide the corresponding Grignard reagents. The presence of bis[2-(dimethylamino)ethyl] ether prevented reduction of the pyrimidine ring and addition by isopropylmagnesium chloride. As a result, the newly formed reactive Grignard reagents were allowed to react with electrophiles in a highly selective manner to afford adducts in excellent yields. In the experimental materials used by the author, we found 3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6Reference of 3-(Pyrimidin-5-yl)benzaldehyde)

3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Reference of 3-(Pyrimidin-5-yl)benzaldehydeThey 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

Related Products of 86443-51-8On May 31, 2017, Jarusiewicz, Jamie A.; Jeon, Jae Yoon; Connelly, Michele C.; Chen, Yizhe; Yang, Lei; Baker, Sharyn D.; Guy, R. Kiplin published an article in ACS Omega. The article was 《Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia》. The article mentions the following:

Profiling of the kinase-binding capabilities of an aminopyrimidine analog detected in a cellular screen of the St. Jude small-mol. collection led to the identification of a novel series of FMS-like tyrosine kinase 3 (FLT3) inhibitors. Structure-activity relationship studies led to the development of compounds exhibiting good potency against MV4-11 and MOLM13 acute myelogenous leukemia cells driven by FLT3, regardless of their FLT3 mutation status. In vitro pharmacol. profiling demonstrated that compound 5e shows characteristics suitable for further preclin. development. The experimental process involved the reaction of 2-Chloro-N-ethylpyrimidin-4-amine(cas: 86443-51-8Related Products of 86443-51-8)

2-Chloro-N-ethylpyrimidin-4-amine(cas: 86443-51-8) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Related Products of 86443-51-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Han, Shuwen; Zhou, Wei; Zhuang, Chunlin; Chen, Fener published an article in Bioorganic Chemistry. The title of the article was 《Structure-Based design of Marine-derived Meridianin C derivatives as glycogen synthase kinase 3β inhibitors with improved oral bioavailability: From aminopyrimidyl-indoles to the sulfonyl analogues》.COA of Formula: C4H2Cl2N2 The author mentioned the following in the article:

Glycogen synthase kinase 3β (GSK-3β) has become an attractive target for the treatment of diabetes. Compound I is an indole-based GSK-3β inhibitor designed from the Meridianin C, a marine natural product (MNP) isolated from Aplidium meridianum. However, this compound has a moderate inhibitory activity toward GSK-3β (IC50 = 24.4 μM), moderate glucose uptake (38%), and especially, a low oral bioavailability (F = 11.4%). In the present study, applying the structure-based design strategy, a series of derivatives modified on the indole moiety were synthesized based on the lead compound I, followed by evaluating their cytotoxic activity, antihyperglycemic activity, and kinase inhibitory activity. Among this series, compound 6x with a sulfonyl group displayed the highest glucose uptake (83.5%) in muscle L6 cells, showing much higher inhibitory activity against GSK-3β (IC50 = 5.25 μM). Mol. docking indicated that compound 6x was properly inserted into the ATP-binding binding pocket of GSK-3β with a higher docking score (-8.145 kcal/mol) compared with that of compound I (-6.950 kcal/mol), interpreting the higher kinase inhibitory activity toward GSK-3β. Remarkably, compound 6x showed favorable drug-like properties, including significantly better oral bioavailability (F = 47.4%) and no two-week acute toxicity at a dose of 1g/kg. Our findings suggest that these MNP-derived sulfonyl indole derivatives could be used as lead compounds for the development of anti-hyperglycemic drugs. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1COA of Formula: 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.COA of Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2014,Gehringer, Matthias; Forster, Michael; Pfaffenrot, Ellen; Bauer, Silke M.; Laufer, Stefan A. published 《Novel hinge-binding motifs for janus kinase 3 inhibitors: a comprehensive structure-activity relationship study on tofacitinib bioisosteres》.ChemMedChem published the findings.Related Products of 90213-66-4 The information in the text is summarized as follows:

The Janus kinases (JAKs) are a family of cytosolic tyrosine kinases crucially involved in cytokine signaling. JAKs have been demonstrated to be valid targets in the treatment of inflammatory and myeloproliferative disorders, and two inhibitors, tofacitinib and ruxolitinib, recently received their marketing authorization. Despite this success, selectivity within the JAK family remains a major issue. Both approved compounds share a common 7H-pyrrolo[2,3-d]pyrimidine hinge binding motif, and little is known about modifications tolerated at this heterocyclic core. In the current study, a library of tofacitinib bioisosteres was prepared and tested against JAK3. The compounds possessed the tofacitinib piperidinyl side chain, whereas the hinge binding motif was replaced by a variety of heterocycles mimicking its pharmacophore. In view of the promising expectations obtained from mol. modeling, most of the compounds proved to be poorly active. However, strategies for restoring activity within this series of novel chemotypes were discovered and crucial structure-activity relationships were deduced. The compounds presented may serve as starting point for developing novel JAK inhibitors and as a valuable training set for in silico models. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Related Products of 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Related Products of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Viswanathan, Kishore; Frey, Kathleen M.; Scocchera, Eric W.; Martin, Brooke D.; Swain, P. Whitney III; Alverson, Jeremy B.; Priestley, Nigel D.; Anderson, Amy C.; Wright, Dennis L. published their research in PLoS One on February 29 ,2012. The article was titled 《Toward new therapeutics for skin and soft tissue infections: propargyl-linked antifolates are potent inhibitors of MRSA and Streptococcus pyogenes》.Category: pyrimidines The article contains the following contents:

Hospital- and community-acquired, complicated skin and soft tissue infections, often attributed to Staphylococcus aureus and Streptococcus pyogenes, present a significant health burden that is associated with increased health care costs and mortality. As these two species are difficult to discern on diagnosis and are associated with differential profiles of drug resistance, the development of an efficacious antibacterial agent that targets both organisms is a high priority. Herein we describe a structure-based drug development effort that has produced highly potent inhibitors of dihydrofolate reductase from both species. Optimized propargyl-linked antifolates containing a key pyridyl substituent display antibacterial activity against both methicillin-resistant S. aureus and S. pyogenes at MIC values below 0.1 μg/mL and minimal cytotoxicity against mammalian cells. Further evaluation against a panel of clin. isolates shows good efficacy against a range of important phenotypes such as hospital- and community-acquired strains as well as strains resistant to vancomycin. In the experiment, the researchers used 3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6Category: pyrimidines)

3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Category: pyrimidinesThey 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

Product Details of 3934-20-1In 2019 ,《Synthesis, Characterization, Anticancer and Antimicrobial Activity Studies of Novel Isomeric 2,4-Disubstituted Ureide Derivatives of Pyrimidinopiperidines》 appeared in ChemistrySelect. The author of the article were Bhavanam, Lourdu Rani; Kotra, Vijay; Mule, Sivanagi Reddy; Krishna Khandapu, Bala Murali; Bollikolla, Hari Babu. The article conveys some information:

A series of isomeric ureide derivatives of novel 2,4-disubstituted pyrimidinopiperidines, e.g., I were synthesized starting from 2,4-dichloropyrimidine. All the final products were purified on silica and characterized by spectral anal. Both the 2,4-disubstituted pyrimidinopiperidines were analyzed for their in vitro anticancer activity on the cell lines HCT116, MIA-PaCa2 and MDA-MB 231 by using MTT cell proliferation assay. Further, the antimicrobial studies were carried out against different bacterial and fungal strains by employing cup plate method. These compounds showed significant anticancer activity on tested three cancer cell lines and exhibited potent antimicrobial activity in tested strains of bacteria and fungi. In addition to this study using 2,4-Dichloropyrimidine, there are many other studies that have used 2,4-Dichloropyrimidine(cas: 3934-20-1Product Details of 3934-20-1) was used in this study.

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.Product Details of 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Nitrogen Enables the Intensity Modulation of Charge Transfer and Spin Paramagnetism in Graphdiyne》 was written by Zhang, Mingjia; Guan, Zhaoyong; Yang, Ze; Hu, Xiuli; Wang, Xiaoxiong; Long, Yun-Ze; Huang, Changshui. Recommanded Product: 2,4,6-Trichloropyrimidine And the article was included in Chemistry of Materials in 2020. The article conveys some information:

The modulation of intrinsic properties, including magnetism in 2-dimensional materials, has attracted considerable interest as it expands device performance and allows for advanced flexible electronics. Herein, a facile way is developed to modulate the magnetic and elec. response of graphdiyne (GDY) by precise N doping. The introduced N exists only as specific pyridine N and can meet the relative change of 1:2:3 between different materials, which can be used as a switch-like property to manipulate charge transfer and spin. Among these, triazine-graphdiyne (TA-GDY) with the most N content achieves the highest saturation magnetization of up to 3.0 emu/g at 2 K. The accompanying moderate band gap and mobility of up to 7.56 cm2 V-1 s-1 endow it a broad application prospect. These results revealed that controllable N doping can modulate the phys. properties of C-based materials, thus providing a critical way to extend their application in future C electronics involving spin. The experimental part of the paper was very detailed, including the reaction process of 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. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Recommanded Product: 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Achieving efficient deep-blue TADF in carbazole-pyrimidine compounds》 was published in Organic Electronics in 2020. These research results belong to Serevicius, Tomas; Skaisgiris, Rokas; Fiodorova, Irina; Steckis, Vytautas; Dodonova, Jelena; Banevicius, Dovydas; Kazlauskas, Karolis; Jursenas, Saulius; Tumkevicius, Sigitas. COA of Formula: C4H2Cl2N2 The article mentions the following:

An approach for achieving deep blue thermally activated delayed fluorescence (TADF) is presented. A simple carbazole-pyrimidine compound Cbz-PYR with near-UV emission and simultaneous room-temperature phosphorescence (RTP) was selectively modified by lowering the singlet state energy, simultaneously preserving high triplet energy. The modified compound tCbz-mPYRs was shown to be efficient TADF emitter with 0.5 solid-state emission yield and peak wavelength of 428 nm. When used in OLED device, tCbz-mPYRs based OLED showed electroluminescence with 8.7% external quantum efficiency (EQE) and Commission Internationale de l′Eclairage (CIE) coordinates of (0.16; 0.12). In the part of experimental materials, we found many familiar compounds, such as 4,6-Dichloropyrimidine(cas: 1193-21-1COA of Formula: C4H2Cl2N2)

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.COA of Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《Phenyl- and Pyrazolyl-Functionalized Pyrimidine: Versatile Chromophore of Bis-Tridentate Ir(III) Phosphors for Organic Light-Emitting Diodes》 were Chen, Yi-Kuang; Kuo, Hsin-Hung; Luo, Dian; Lai, Yi-Ning; Li, Wei-Cheng; Chang, Chih-Hao; Escudero, Daniel; Jen, Alex K.-Y.; Hsu, Ling-Yang; Chi, Yun. And the article was published in Chemistry of Materials in 2019. Recommanded Product: 3764-01-0 The author mentioned the following in the article:

There is growing interest in the bis-tridentate Ir(III) emitters as they are expected to display both improved emission efficiency and improved photostability. Herein, the authors turned to the new emitters m2h-1-3 and m6h-1-3, bearing a pincer carbene ancillary and a chromophoric chelate derived from judiciously selected phenyl-pyrimidine-pyrazole entities (pzm2hF)H2 and (pzm6hF)H2, which differ in terms of the location of Ph and pyrazole substituents on the central pyrimidine. D. functional theory calculations revealed a notable change in the spin d. distribution from the pyrimidine-pyrazolate entity in m2h to the pyrimidine-Ph fragment in m6h. As a consequence, the m6h emitters exhibited both shortened emission lifetimes and improved stabilities during extensive photolysis in solution, while corresponding organic light-emitting diodes (OLEDs) doped with green-emitting m6h-1 and sky-blue-emitting m6h-2 and m6h-3 exhibited external quantum efficiencies of 17.6, 15.9, and 17.6%, resp., superior to those of all of their m2h counterparts at a practical luminance of 103 cd/m2. This finding suggests a new methodol. for fine-tuning the electronic transition that is important to high-performance and durable phosphorescent OLEDs. In the experimental materials used by the author, we found 2,4,6-Trichloropyrimidine(cas: 3764-01-0Recommanded Product: 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.Recommanded Product: 3764-01-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Gower, Carrie M.; Thomas, Jason R.; Harrington, Edmund; Murphy, Jason; Chang, Matthew E. K.; Cornella-Taracido, Ivan; Jain, Rishi K.; Schirle, Markus; Maly, Dustin J. published 《Conversion of a Single Polypharmacological Agent into Selective Bivalent Inhibitors of Intracellular Kinase Activity》.ACS Chemical Biology published the findings.Product Details of 3764-01-0 The information in the text is summarized as follows:

Loss-of-function studies are valuable for elucidating kinase function and the validation of new drug targets. While genetic techniques, such as RNAi and genetic knockouts, are highly specific and easy to implement, in many cases post-translational perturbation of kinase activity, specifically pharmacol. inhibition, is preferable. However, due to the high degree of structural similarity between kinase active sites and the large size of the kinome, identification of pharmacol. agents that are sufficiently selective to probe the function of a specific kinase of interest is challenging, and there is currently no systematic method for accomplishing this goal. Here, the authors present a modular chem. genetic strategy that uses antibody mimetics as highly selective targeting components of bivalent kinase inhibitors. The authors demonstrate that it is possible to confer high kinase selectivity to a promiscuous ATP-competitive inhibitor by tethering it to an antibody mimetic fused to the self-labeling protein SNAPtag. With this approach, a potent bivalent inhibitor of the tyrosine kinase Abl was generated. Profiling in complex cell lysates, with competition-based quant. chem. proteomics, revealed that this bivalent inhibitor possesses greatly enhanced selectivity for its target, BCR-Abl, in K562 cells. Importantly, the authors show that both components of the bivalent inhibitor can be assembled in K562 cells to block the ability of BCR-Abl to phosphorylate a direct cellular substrate. Finally, the authors demonstrate the generality of using antibody mimetics as components of bivalent inhibitors by generating a reagent that is selective for the activated state of the serine/threonine kinase ERK2. The results came from multiple reactions, including the reaction of 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. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Product Details of 3764-01-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia