Day: October 17, 2022

Sakamoto, Takao; Satoh, Chisato; Kondo, Yoshinori; Yamanaka, Hiroshi published an article on January 31 ,1993. The article was titled 《Condensed heteroaromatic ring systems. XXI. Synthesis of pyrrolo[2,3-d]pyrimidines and pyrrolo[3,2-d]pyrimidines》, and you may find the article in Chemical & Pharmaceutical Bulletin.Category: pyrimidines The information in the text is summarized as follows:

The title compounds, e.g., I and II were synthesized in high yields by the palladium-catalyzed reaction of 4-acetylamino-5-bromopyrimidines and 5-acetylamino-4-iodopyrimidines with (Z)-1-ethoxy-2-(tributylstannyl)ethene followed by cyclization under acidic conditions.4-Chloro-6-methoxy-5-nitropyrimidine(cas: 52854-14-5Category: pyrimidines) was used in this study.

4-Chloro-6-methoxy-5-nitropyrimidine(cas: 52854-14-5) 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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2014,O’Brien, Nathan J.; Brzozowski, Martin; Buskes, Melissa J.; Deady, Leslie W.; Abbott, Belinda M. published 《Synthesis and biological evaluation of 2-anilino-4-substituted-7H-pyrrolopyrimidines as PDK1 inhibitors》.Bioorganic & Medicinal Chemistry published the findings.Category: pyrimidines The information in the text is summarized as follows:

3-Phosphoinositide-dependent kinase 1 (PDK1), a biol. target that has attracted a large amount of attention recently, is responsible for the pos. regulation of the PI3K/Akt pathway that is often activated in a large number of human cancers. A series of second-generation 2-anilino-4-substituted-7H-pyrrolopyrimidines were synthesized by installation of various functions at the 4-position of the 7H-pyrrolopyrimidine scaffold. All compounds were screened against the isolated PDK1 enzyme and dose response anal. was obtained on the best compounds of the series.2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Category: pyrimidines) was used in this study.

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. Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,Ding, Xiao; Stasi, Luigi Piero; Ho, Ming-Hsun; Zhao, Baowei; Wang, Hailong; Long, Kai; Xu, Qiongfeng; Sang, Yingxia; Sun, Changhui; Hu, Huan; Yu, Haihua; Wan, Zehong; Wang, Lizhen; Edge, Colin; Liu, Qian; Li, Yi; Dong, Kelly; Guan, Xiaoming; Tattersall, F. David; Reith, Alastair D.; Ren, Feng published 《Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.HPLC of Formula: 90213-66-4 The information in the text is summarized as follows:

Inhibition of LRRK2 kinase activity with small mols. has emerged as a potential novel therapeutic treatment for Parkinson’s disease. Herein the authors disclose the discovery of a 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amine series as potent LRRK2 inhibitors identified through a kinase-focused set screening. Optimization of the physicochem. properties and kinase selectivity led to the discovery of compound 7 ((4-((4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone), which exhibited potent in vitro inhibition of LRRK2 kinase activity, good physicochem. properties and kinase selectivity across the kinome. Moreover, compound 7 was able to penetrate into the CNS, and in vivo pharmacol. studies revealed significant inhibition of Ser 935 phosphorylation in the brain of both rats (30 and 100 mg/kg) and mice (45 mg/kg) following oral administration. After reading the article, we found that the author used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4HPLC of Formula: 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. HPLC of Formula: 90213-66-4They 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

The author of 《Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors》 were Rowlands, Rachel A.; Cato, M. Claire; Waldschmidt, Helen V.; Bouley, Renee A.; Chen, Qiuyan; Avramova, Larisa; Larsen, Scott D.; Tesmer, John J. G.; White, Andrew D.. And the article was published in ACS Medicinal Chemistry Letters in 2019. Application In Synthesis of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The author mentioned the following in the article:

The ability of G protein-coupled receptor (GPCR) kinases (GRKs) to regulate desensitization of GPCRs has made GRK2 and GRK5 attractive targets for treating heart failure and other diseases such as cancer. Although advances have been made toward developing inhibitors that are selective for GRK2, there have been far fewer reports of GRK5 selective compounds Herein, we describe the development of GRK5 subfamily selective inhibitors, 5 and 16d that covalently interact with a nonconserved cysteine (Cys474) unique to this subfamily. Compounds 5 and 16d feature a highly amenable pyrrolopyrimidine scaffold that affords high nanomolar to low micromolar activity that can be easily modified with Michael acceptors with various reactivities and geometries. Our work thereby establishes a new pathway toward further development of subfamily selective GRK inhibitors and establishes Cys474 as a new and useful covalent handle in GRK5 drug discovery. The results came from multiple reactions, including the reaction of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Application In Synthesis of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) 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 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidineThey 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

Toviwek, Borvornwat; Phuangsawai, Oraphan; Konsue, Adchatawut; Hannongbua, Supa; Riley, Jennifer; Mutter, Nicole; Anderson, Mark; Webster, Lauren; Hallyburton, Irene; Read, Kevin D.; Gleeson, M. Paul published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Preparation, biological & cheminformatics-based assessment of N2,N4-diphenylpyrimidine-2,4-diamine as potential Kinase-targeted antimalarials》.Application In Synthesis of 2,4-Dichloropyrimidine The article contains the following contents:

Twenty eight new N2,N4-diphenylpyrimidine-2,4-diamines have been prepared in order to expand our understanding of the anti-malarial SAR of the scaffold. The aim of the study was to make structural modifications to improve the overall potency, selectivity and solubility of the series by varying the anilino groups attached to the 2- and 4-position. We evaluated the activity of the compounds against Plasmodium falciparum (Pf) 3D7, cytotoxicity against HepG2, % inhibition at a panel of 10 human kinases, solubility, permeability and lipophilicity, and human and rat in vitro clearance. 11 was identified as a potent anti-malarial with an IC50 of 0.66 μM at the 3D7 strain and a selectivity (SI) of ∼ 40 in terms of cytotoxicity against the HepG2 cell line. It also displayed low exptl. logD7.4 (2.27), reasonable solubility (124 μg/mL), good metabolic stability, but low permeability. A proteo-chemometric workflow was employed to identify putative Pf targets of the most promising compounds Ligand-based similarity searching of the ChEMBL database led to the identification of most probable human targets. These were then used as input for sequence-based searching of the Pf proteome. Homol. modeling and mol. docking were used to evaluate whether compounds could indeed bind to these targets with valid binding modes. In vitro biol. testing against close human analogs of these targets was subsequently undertaken. This allowed us to identify potential Pf targets and human anti-targets that could be exploited in future development. In the part of experimental materials, we found many familiar compounds, such as 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

Sharma, Lalit Kumar; Yun, Mi Kyung; Subramanian, Chitra; Tangallapally, Rajendra; Jackowski, Suzanne; Rock, Charles O.; White, Stephen W.; Lee, Richard E. published an article in 2021. The article was titled 《LipE guided discovery of isopropylphenyl pyridazines as pantothenate kinase modulators》, and you may find the article in Bioorganic & Medicinal Chemistry.Category: pyrimidines The information in the text is summarized as follows:

Pantothenate kinase (PANK) is the critical regulator of intracellular levels of CoA and has emerged as an attractive target for treating neurol. and metabolic disorders. This report describes the optimization, synthesis, and full structure-activity relationships of a new chem. series of pantothenate competitive PANK inhibitors. Potent drug-like mols. were obtained by optimizing a high throughput screening hit, using lipophilic ligand efficiency (LipE) derived from human PANK3 IC50 values to guide ligand development. X-ray crystal structures of PANK3 with index inhibitors from the optimization were determined to rationalize the emerging structure activity relationships. The anal. revealed a key bidentate hydrogen bonding interaction between pyridazine and R306′ as a major contributor to the LipE gain observed in the optimization. A tractable series of PANK3 modulators with nanomolar potency, excellent LipE values, desirable physicochem. properties, and a well-defined structural binding mode was produced from this study. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Category: pyrimidines)

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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Quality Control of 4,6-DichloropyrimidineIn 2020 ,《Ruthenium, rhodium and iridium complexes containing pyrimidine based thienyl pyrazoles: Synthesis and antibacterial studies》 was published in Journal of Organometallic Chemistry. The article was written by Lapasam, Agreeda; Mawnai, Ibaniewkor L.; Banothu, Venkanna; Kaminsky, Werner; Kollipara, Mohan Rao. The article contains the following contents:

The reaction of pyrimidine based electron-rich heterocyclic thiophene pyrazoles and halide bridged arene d6 metal precursors yielded a series of mononuclear and dinuclear half sandwich d6 metal complexes. Mononuclear and dinuclear complexes formed by the ratio-based reaction between ligand and metal precursor. All these cationic complexes have been characterized by IR, UV-Vis, 1H NMR, 13C NMR spectroscopic techniques. Complex 5 has been established by single-crystal anal. X-ray diffraction studies revealed the formation of mononuclear and dinuclear complexes and suggest that the vicinity around the metal atom is distorted octahedral. An in vitro study to screen the antibacterial potential of these complexes against pathogenic bacteria, S. aureus, K. pneumoniae, and E. coli was addressed. All the complexes display a better zone of inhibitions for both Gram-pos. (S. aureus) and Gram-neg. strains (K. pneumoniae, and E. coli). The min. inhibitory concentrations (MICs) for the most active complex ranged from 0.125 to 0.25 mg/mL for S. aureus and Klebsiella Pneumoniae and 0.25-0.5 mg/mL for E. coli. The experimental part of the paper was very detailed, including the reaction process of 4,6-Dichloropyrimidine(cas: 1193-21-1Quality Control of 4,6-Dichloropyrimidine)

4,6-Dichloropyrimidine(cas: 1193-21-1) 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.Quality Control of 4,6-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 1193-21-1In 2020 ,《Achieving Submicrosecond Thermally Activated Delayed Fluorescence Lifetime and Highly Efficient Electroluminescence by Fine-Tuning of the Phenoxazine-Pyrimidine Structure》 was published in ACS Applied Materials & Interfaces. The article was written by Serevicius, Tomas; Skaisgiris, Rokas; Dodonova, Jelena; Jagintavicius, Laimis; Banevicius, Dovydas; Kazlauskas, Karolis; Tumkevicius, Sigitas; Jursenas, Saulius. The article contains the following contents:

Thermally activated delayed fluorescence (TADF) materials, combining high fluorescence quantum efficiency and short delayed emission lifetime, are highly desirable for application in organic light-emitting diodes (OLEDs) with negligible external quantum efficiency (EQE) roll-off. Here, we present the pathway for shortening the TADF lifetime of highly emissive 4,6-bis[4-(10-phenoxazinyl)phenyl]pyrimidine derivatives Tiny manipulation of the mol. structure with Me groups was applied to tune the singlet-triplet energy-level scheme and the corresponding coupling strengths, enabling the boost of the reverse intersystem crossing (rISC) rate (from 0.7 to 6.5) × 106 s-1 and shorten the TADF lifetime down to only 800 ns in toluene solutions An almost identical TADF lifetime of roughly 860 ns was attained also in solid films for the compound with the most rapid TADF decay in toluene despite the presence of inevitable conformational disorder. Concomitantly, the boost of fluorescence quantum efficiency to near unity was achieved in solid films due to the weakened nonradiative decay. Exceptional EQE peak values of 26.3-29.1% together with adjustable emission wavelength in the range of 502-536 nm were achieved in TADF OLEDs. Reduction of EQE roll-off was demonstrated by lowering the TADF lifetime. In the experiment, the researchers used many compounds, for example, 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 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.Related Products of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《1,2,3-Thiadiazolo[5,4-b]pyrimidin-4(5H)ones》 was published in Journal of Heterocyclic Chemistry in 1976. These research results belong to Hymans, William E.. Related Products of 6237-96-3 The article mentions the following:

Potential herbicides I (R = Et, Pr, CHMe2, Bu, CH2CHMe2, CMe3, CH2CMe3) were prepared in 6 steps from RC(:NH)NH2 and CH2(CO2Et)2. In addition to this study using 4,6-Dichloro-2-ethylpyrimidin-5-amine, there are many other studies that have used 4,6-Dichloro-2-ethylpyrimidin-5-amine(cas: 6237-96-3Related Products of 6237-96-3) was used in this study.

4,6-Dichloro-2-ethylpyrimidin-5-amine(cas: 6237-96-3) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Related Products of 6237-96-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Formula: C6H6BrClN2On October 31, 1989 ,《Studies on pyrimidine derivatives. XLI. Palladium-catalyzed cross-coupling reaction of halopyrimidines with aryl- and vinyltributylstannanes》 appeared in Chemical & Pharmaceutical Bulletin. The author of the article were Kondo, Yoshinori; Watanabe, Ryo; Sakamoto, Takao; Yamanaka, Hiroshi. The article conveys some information:

The arylation of 2-, 4-, and 5-halopyrimidines with aryltributylstannanes in the presence of dichlorobis(triphenylphosphine)palladium was investigated with successful results. The reaction can be expanded to the synthesis of 2-, 4-, and 5-vinylpyrimidines with generality. Thus the reaction of pyrimidine I (R = Cl) with R1SnBu3 (R1 = Ph, 2-thienyl, vinyl) gave I (R = R1). After reading the article, we found that the author used 5-Bromo-4-chloro-2,6-dimethylpyrimidine(cas: 69696-35-1Formula: C6H6BrClN2)

5-Bromo-4-chloro-2,6-dimethylpyrimidine(cas: 69696-35-1) 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.Formula: C6H6BrClN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia