Month: October 2022

Product Details of 6297-80-9On November 1, 2012 ,《Discovery of phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Giordanetto, Fabrizio; Waallberg, Andreas; Ghosal, Saswati; Iliefski, Tommy; Cassel, Johan; Yuan, Zhong-Qing; von Wachenfeldt, Henrik; Andersen, Soeren M.; Inghardt, Tord; Tunek, Anders; Nylander, Sven. The article conveys some information:

Structure-based evolution of the original fragment leads resulted in the identification of 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, (S)-21, a potent, selective phosphoinositide 3-kinases (PI3K) p110β isoform inhibitor with favorable in vivo antiplatelet effect. Despite its antiplatelet action, (S)-21 did not significantly increase bleeding time in dogs. Addnl., due to its enhanced selectivity over p110α, (S)-21 did not induce any insulin resistance in rats. In addition to this study using 4,6-Dichloropyrimidin-2(1H)-one, there are many other studies that have used 4,6-Dichloropyrimidin-2(1H)-one(cas: 6297-80-9Product Details of 6297-80-9) was used in this study.

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.Product Details of 6297-80-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1987,Biochemical and Clinical Aspects of Pteridines included an article by Huebsch, Walter. HPLC of Formula: 6297-80-9. The article was titled 《Synthesis and biological activity of 8-substituted thiolumazines》. The information in the text is summarized as follows:

I (X and Y = O or S, R = Me, CH2CH2OH, Ph, or ribityl were prepared as precursors and converted to thiolumazine derivatives II (X and Y = O or S, R = Me, CH2CH2OH, Ph, or ribityl, R1 and R2 = H, Me, OH, or Ph) were prepared and then structure-activity relation discussed with regard to enzyme inhibition in chemotherapy. The 2-oxo group was important for enzyme substrate interaction. Replacement by S had a strong neg. effect. In addition to this study using 4,6-Dichloropyrimidin-2(1H)-one, there are many other studies that have used 4,6-Dichloropyrimidin-2(1H)-one(cas: 6297-80-9HPLC of Formula: 6297-80-9) was used in this study.

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.HPLC of Formula: 6297-80-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1984,Kazimierczuk, Zygmunt; Cottam, Howard B.; Revankar, Ganapathi R.; Robins, Roland K. published 《Synthesis of 2′-deoxytubercidin, 2′-deoxyadenosine, and related 2′-deoxynucleosides via a novel direct stereospecific sodium salt glycosylation procedure》.Journal of the American Chemical Society published the findings.Recommanded Product: 90213-66-4 The information in the text is summarized as follows:

A general and stereospecific synthesis has been developed for the direct preparation of 2′-deoxy-β-D-ribofurnaosylpurine analogs including 2′-deoxyadenosine derivatives The reaction of the Na salt of chloropyrrolo[2,3-d]pyrimidines I (R = H, Cl) with 1-chloro-2-deoxy-3,5-di-O-p-toluoyl-α-D-erythro-pentofuranose (II) provided the corresponding N-1 2′-deoxy-β-D-ribofuranosyl blocked derivatives which, on ammonolysis, gave 2′-deoxytubercidin (III, R = H) and 2-chloro-2′-deoxyrubercidin (III, R = Cl), resp., in good yields. This glycosylation also readily proceeds in the presence of a 2-methylthio group. Application of this glycosylation procedure to 4,6-dichloroimidazo[4,5-c]pyridine, 6-chloropurine, 2,6-dichloropurine, and 4-chloropyrazolo[3,4-d]pyrimidine gave 2-chloro-2′-deoxy-3-deazaadenosine, 2′-deoxyadenosine, 2-chloro-2′-deoxyadenosine, and 4-amino-1-(2-deoxy-β-D-erythro-pentofuranosyl)pyrazolo[3,4-d]pyrimidine, resp. Similarly, glycosylation and ammonolysis of 4,6-dichloro-1H-pyrrolo[3,2-c]pyridine gave 4,6-dichloro-1-(2-deoxy-β-D-erythro-pentofuranosyl)pyrrolo[3,2-c]pyridine. This stereospecific attachment of the 2-deoxy-β-D-ribofuranosyl moiety appears to be due to a Walden inversion at the C-1 carbon of II. The results came from multiple reactions, including the reaction of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Recommanded Product: 90213-66-4)

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2014,Rodriguez, Rodrigo A.; Pan, Chung-Mao; Yabe, Yuki; Kawamata, Yu; Eastgate, Martin D.; Baran, Phil S. published 《Palau’chlor: A Practical and Reactive Chlorinating Reagent》.Journal of the American Chemical Society published the findings.Product Details of 90213-66-4 The information in the text is summarized as follows:

Unlike its other halogen atom siblings, the utility of chlorinated arenes and (hetero)arenes are twofold: they are useful in tuning electronic structure as well as acting as points for diversification via cross-coupling. Herein we report the invention of a new guanidine-based chlorinating reagent I, CBMG or “”Palau’chlor””, inspired by a key chlorospirocyclization en route to pyrrole imidazole alkaloids. This direct, mild, operationally simple, and safe chlorinating method is compatible with a range of nitrogen-containing heterocycles as well as select classes of arenes, conjugated π-systems, sulfonamides, and silyl enol ethers. Comparisons with other known chlorinating reagents revealed CBMG to be the premier reagent. After reading the article, we found that the author used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Product Details of 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) 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. Product Details of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Kim, Juae; Shim, Joo Young; Lee, Jihoon; Lee, Dal Yong; Chae, Sangmin; Kim, Jinwoo; Kim, Il; Kim, Hyo Jung; Park, Sung Heum; Suh, Hongsuk published 《Syntheses of pyrimidine-based polymers containing electron-withdrawing substituent with high open circuit voltage and applications for polymer solar cells》.Journal of Polymer Science, Part A: Polymer Chemistry published the findings.Related Products of 3764-01-0 The information in the text is summarized as follows:

Polymers using new electron-deficient units, 2-pyriminecarbonitrile and 2-fluoropyrimidine, were synthesized and utilized for the photovoltaics. Donor-acceptor (D-A) types of conjugated polymers (PBDTCN, PBDTTCN, PBDTF, and PBDTTF) containing 4,8-bis(2-octyldodecyloxy)benzo[1,2-b;3,4-b’]dithiophene (BDT) or 4,8-bis(5-(2-octyldodecyloxy)thiophen-2-yl)benzo[1,2-b:4,5-b’]dithiophene (BDTT) as electron rich unit and 2-pyriminecarbonitrile or 2-fluoropyrimidine as electron deficient unit were synthesized. We designed pyrimidine derivatives in which strong electron-withdrawing group (CN or fluorine) was introduced to the C2 position for the generation of strong electron-deficient property. By the combination with the electron-rich unit, the pyrimidines will provide low band gap polymers with low HOMO energy levels for higher open-circuit voltages (VOC). For the syntheses of the polymers, the electron-rich and the electron-deficient units were combined by Stille coupling reaction with Pd(0)-catalyst. Absorption spectra of the thin films of PBDTTCN and PBDTTF with BDTT unit show shift to a longer wavelength region than PBDTCN and PBDTF with BDT unit. Four synthesized polymers provided low electrochem. bandgaps of 1.56 to 1.96 eV and deep HOMO energy levels between -5.67 and -5.14 eV. © 2015 The Authors. Journal of Polymer Science Part A: Polymer Chem. Published by Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2015. The results came from multiple reactions, including the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products 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.Related Products of 3764-01-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《A chemoproteomic strategy for direct and proteome-wide covalent inhibitor target-site identification》 were Browne, Christopher M.; Jiang, Baishan; Ficarro, Scott B.; Doctor, Zainab M.; Johnson, Jared L.; Card, Joseph D.; Sivakumaren, Sindhu Carmen; Alexander, William M.; Yaron, Tomer M.; Murphy, Charles J.; Kwiatkowski, Nicholas P.; Zhang, Tinghu; Cantley, Lewis C.; Gray, Nathanael S.; Marto, Jarrod A.. And the article was published in Journal of the American Chemical Society in 2019. Recommanded Product: 2,4-Dichloropyrimidine The author mentioned the following in the article:

Despite recent clin. successes for irreversible drugs, potential toxicities mediated by unpredictable modification of off-target cysteines represents a major hurdle for expansion of covalent drug programs. Understanding the proteome-wide binding profile of covalent inhibitors can significantly accelerate their development; however, current mass spectrometry strategies typically do not provide a direct, amino acid level readout of covalent activity for complex, selective inhibitors. Here we report the development of CITe-Id, a novel chemoproteomic approach that employs covalent pharmacol. inhibitors as enrichment reagents in combination with an optimized proteomic platform to directly quantify dose-dependent binding at cysteine-thiols across the proteome. CITe-Id anal. of our irreversible CDK inhibitor THZ1 identified dose-dependent covalent modification of several unexpected kinases, including a previously unannotated cysteine (C840) on the understudied kinase PKN3. These data streamlined our development of JZ128 as a new selective covalent inhibitor of PKN3. Using JZ128 as a probe compound, we identified novel potential PKN3 substrates, thus offering an initial mol. view of PKN3 cellular activity. CITe-Id provides a powerful complement to current chemoproteomic platforms to characterize the selectivity of covalent inhibitors, identify new, pharmacol. addressable cysteine-thiols, and inform structure-based drug design programs. After reading the article, we found that the author used 2,4-Dichloropyrimidine(cas: 3934-20-1Recommanded Product: 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.Recommanded Product: 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Safety of 4,6-DichloropyrimidineIn 2019 ,《Synthesis, pharmacological characterization, and structure-activity relationships of non-canonical selective agonists for α7 nAChRs》 appeared in Journal of Medicinal Chemistry. The author of the article were Camacho-Hernandez, Gisela Andrea; Stokes, Clare; Duggan, Brendan M.; Kaczanowska, Katarzyna; Brandao-Araiza, Stefania; Doan, Lisa; Papke, Roger L.; Taylor, Palmer. The article conveys some information:

Noncanonical 2,4,6-substituted pyrimidine analogs were prepared for a structure-activity relationship study. The new lead compounds activate selectively the α7 nAChRs with EC50’s between 30-140 nM in a PNU-120596-dependent, cell-based calcium influx assay. After characterizing the expanded lead landscape, author ranked the compounds for rapid activation using Xenopus oocytes expressing human α7 nAChR with a two-electrode voltage clamp. This approach enabled us to define the mol. determinants governing rapid activation, agonist potency, and desensitization of α7 nAChRs after exposure to pyrimidine analogs, thereby distinguishing this subclass of non-canonical agonists from previously defined types of agonists (agonists, partial agonists, silent agonists, and ago-PAMs). By NMR, author analyzed pKa values for ionization of lead candidates, demonstrating distinctive modes of interaction for this landscape of ligands. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1Safety 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.Safety of 4,6-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Calderwood, David J.; Johnston, David N.; Munschauer, Rainer; Rafferty, Paul published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck》.Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine The author mentioned the following in the article:

A series of pyrrolo[2,3-d]pyrimidines was synthesized and structure-activity relationship was evaluated as inhibitors of Lck. Lck accommodates a diverse set of substituents at N-7. Altering the substituent at N-7 provided another compound, an orally available lck inhibitor which inhibited TCR mediated IL-2 production after oral dosing. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine)

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.Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Michellys, Pierre-Yves; Chen, Bei; Jiang, Tao; Jin, Yunho; Lu, Wenshuo; Marsilje, Thomas H.; Pei, Wei; Uno, Tetsuo; Zhu, Xuefeng; Wu, Baogen; Nguyen, Truc Ngoc; Bursulaya, Badry; Lee, Christian; Li, Nanxin; Kim, Sungjoon; Tuntland, Tove; Liu, Bo; Sun, Frank; Steffy, Auzon; Hood, Tami published 《Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor superfamily. Expression of ALK in normal human tissues is only found in a subset of neural cells, however it is involved in the genesis of several cancers through genetic aberrations involving translocation of the kinase domain with multiple fusion partners (e.g., NPM-ALK in anaplastic large cell lymphoma ALCL or EML4-ALK in non-small cell lung cancer) or activating mutations in the full-length receptor resulting in ligand-independent constitutive activation (e.g., neuroblastoma). Here we are reporting the discovery of novel and selective anaplastic lymphoma kinase inhibitors from specific modifications of the 2,4-diaminopyridine core present in TAE684 and LDK378. Synthesis, structure activity relationships (SAR), absorption, distribution, metabolism, and excretion (ADME) profile, and in vivo efficacy in a mouse xenograft model of anaplastic large cell lymphoma are described. In addition to this study using 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine, there are many other studies that have used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine) was used in this study.

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) 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. Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineOn September 30, 2012 ,《Use of kinase inhibitors to correct ΔF508-CFTR function》 was published in Molecular and Cellular Proteomics. The article was written by Trzcinska-Daneluti, Agata M.; Nguyen, Leo; Jiang, Chong; Fladd, Christopher; Uehling, David; Prakesch, Michael; Al-Awar, Rima; Rotin, Daniela. The article contains the following contents:

The most common mutation in cystic fibrosis (CF) is a deletion of Phe at position 508 (ΔF508-CFTR). ΔF508-CFTR is a trafficking mutant that is retained in the ER, unable to reach the plasma membrane. To identify compounds and drugs that rescue this trafficking defect, we screened a kinase inhibitor library enriched for small mols. already in the clinic or in clin. trials for the treatment of cancer and inflammation, using our recently developed high-content screen technol. The top hits of the screen were further validated by (1) biochem. anal. to demonstrate the presence of mature (Band C) ΔF508-CFTR, (2) flow cytometry to reveal the presence of ΔF508-CFTR at the cell surface, (3) short-circuit current (Isc) anal. in Ussing chambers to show restoration of function of the rescued ΔF508-CFTR in epithelial MDCK cells stably expressing this mutant (including EC50 determinations), and importantly (4) Isc anal. of Human Bronchial Epithelial (HBE) cells harvested from homozygote ΔF508-CFTR transplant patients. Interestingly, several inhibitors of receptor Tyr kinases (RTKs), such as SU5402 and SU6668 (which target FGFRs, VEGFR, and PDGFR) exhibited strong rescue of ΔF508-CFTR, as did several inhibitors of the Ras/Raf/MEK/ERK or p38 pathways (e.g. (5Z)-7-oxozeaenol). Prominent rescue was also observed by inhibitors of GSK-3β (e.g. GSK-3β Inhibitor II and Kenpaullone). These results identify several kinase inhibitors that can rescue ΔF508-CFTR to various degrees, and suggest that use of compounds or drugs already in the clinic or in clin. trials for other diseases can expedite delivery of treatment for CF patients. The experimental part of the paper was very detailed, including the reaction process of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine)

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. Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia