Day: October 20, 2022

《Efficient transformation of thymidine into 2′,3′-didehydro-2′,3′-dideoxythymidine (D4T) involving opening of a 2,3′-anhydro derivative by phenylselenol》 was written by Becouarn, Stefan; Czernecki, Stanislas; Valery, Jean-Marc. Application In Synthesis of ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate And the article was included in Nucleosides & Nucleotides on August 31 ,1995. The article conveys some information:

A high-yielding method for the introduction of the phenylselenyl residue at the 3′-position of thymidine is reported. This reaction avoided any strongly basic or reductive reagent, thus allowing the use of benzoate ester as a protective group at O-5′. Further oxidation-elimination sequence followed by basic deprotection afforded D4T in 67.5% overall yield from thymidine. In the experimental materials used by the author, we found ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9Application In Synthesis of ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate)

((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate(cas: 122567-97-9) 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.Application In Synthesis of ((2S,5R)-5-(5-Methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl benzoate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Category: pyrimidinesOn March 12, 1982, Barczynski, P.; Van der Plas, H. C. published an article in Journal of Organic Chemistry. The article was 《Ring transformations in reactions of heterocyclic compounds with nucleophiles. Part 24. Pyrimidines. Part 86. Conversion of 5-nitropyrimidine into 2-substituted 5-nitropyrimidine and 2-amino-5-nitropyridines by amidines》. The article mentions the following:

The reaction of 5-nitropyrimidine (I) with benzamidine, pivalamidine, acetamidine, propionamidine, α-phenylacetamidine, O-methylisourea hydrochlorides, and cyanamide in ethanolic solution in the presence of Et3N was investigated. I and alkyl(aryl)amidines, having no active methylene groups attached to the amidine moiety (pivalamidine, benzamidine), gave the corresponding 2-substituted 5-nitropyrimidines in good yields. With acetamidine and propionamidine, 2-amino-5-nitropyridines were also formed; with α-phenylacetamidine a 2-amino-5-nitropyridine derivative was obtained exclusively. The reaction of I with both O-methylisourea and cyanamide leads to 2-amino-5-nitropyrimidine. These reactions provide new examples of degenerate ring transformations of the pyrimidine ring system and of the ring transformation of pyrimidines into pyridines. After reading the article, we found that the author used 2-Methoxy-5-nitropyrimidine(cas: 14001-69-5Category: pyrimidines)

2-Methoxy-5-nitropyrimidine(cas: 14001-69-5) is a member of ether. When aromatic ethers are exposed to halogen in the presence or absence of a catalyst, they undergo halogenation, such as bromination.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

HPLC of Formula: 519032-07-6On May 3, 2007 ,《Dihydroxypyrimidine-4-carboxamides as Novel Potent and Selective HIV Integrase Inhibitors》 appeared in Journal of Medicinal Chemistry. The author of the article were Pace, Paola; Di Francesco, M. Emilia; Gardelli, Cristina; Harper, Steven; Muraglia, Ester; Nizi, Emanuela; Orvieto, Federica; Petrocchi, Alessia; Poma, Marco; Rowley, Michael; Scarpelli, Rita; Laufer, Ralph; Gonzalez Paz, Odalys; Monteagudo, Edith; Bonelli, Fabio; Hazuda, Daria; Stillmock, Kara A.; Summa, Vincenzo. The article conveys some information:

Human immunodeficiency virus type-1 (HIV-1) integrase, one of the three constitutive viral enzymes required for replication, is a rational target for chemotherapeutic intervention in the treatment of AIDS that has also recently been confirmed in the clin. setting. We report here on the design and synthesis of N-benzyl-5,6-dihydroxypyrimidine-4-carboxamides as a class of agents which exhibits potent inhibition of the HIV-integrase-catalyzed strand transfer process. In the current study, structural modifications on these mols. were made in order to examine effects on HIV-integrase inhibitory potencies. One of the most interesting compounds for this series is 2-[1-(dimethylamino)-1-methylethyl]-N-(4-fluorobenzyl)-5,6-dihydroxypyrimidine-4-carboxamide, with a CIC95 of 78 nM in the cell-based assay in the presence of serum proteins. The compound has favorable pharmacokinetic properties in preclin. species (rats, dogs, and monkeys) and shows no liabilities in several counterscreening assays, highlighting its potential as a clin. useful antiviral agent. The experimental process involved the reaction of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6HPLC of Formula: 519032-07-6)

Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6) 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: 519032-07-6They 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

Arnold, Zdzislaw; Draminski, Marcin; Fiszer, Bernard published an article in Polish Journal of Chemistry. The title of the article was 《Synthesis of quaternary pyrimidine bases, potential cholinesterase reactivators》.Related Products of 1073-65-0 The author mentioned the following in the article:

The title compounds I (R = Me, Et, Bu, X = I; R = Pr, allyl, X = Br) were obtained in 9-94% yields by quaternization of the oxime by RX in Me2CO 5-60 h at 37°. I showed no activity as cholinesterase reactivators. The results came from multiple reactions, including the reaction of Pyrimidine-4-carbaldehyde oxime(cas: 1073-65-0Related Products of 1073-65-0)

Pyrimidine-4-carbaldehyde oxime(cas: 1073-65-0) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.Related Products of 1073-65-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1971,Journal of Medicinal Chemistry included an article by Cohen, Sasson; Ashani, Yacov. COA of Formula: C5H5N3O. The article was titled 《Nucleophilicity of some reactivators of phosphorylated acetylcholinesterase. 5》. The information in the text is summarized as follows:

Reactivation of diisopropyl phosphorofluoridate-inactivated acetylcholinesterase by 14 heterocyclic oximes, was related with the nucleophilicity and basicity of these oximes. The value of kr (the 1st-order rate constant) at pH 7.4 was a function of both the nucleophilicity of the reactor mol., and its basicity, reaching an optimum for compounds with a pKa value in the range of 7.6-8.0, e.g., 1-methyl-4-formylrimidinium oxime iodide (I). The experimental process involved the reaction of Pyrimidine-4-carbaldehyde oxime(cas: 1073-65-0COA of Formula: C5H5N3O)

Pyrimidine-4-carbaldehyde oxime(cas: 1073-65-0) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.COA of Formula: C5H5N3O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Oppenlaender, Thomas; Pfoertner, Karl Heinz; Schoenholzer, Peter published an article in Helvetica Chimica Acta. The title of the article was 《Photooxygenation of 5-aryl-2,4-diaminopyrimidines leading to 4-amino-1,3,5-triazin-2-yl ketones and, in the presence of sodium borohydride, to 5,6-dihydro-4(3H)-pyrimidinones》.Related Products of 15400-54-1 The author mentioned the following in the article:

The photosensitized oxygenation of 5-aryl-2,4-diaminopyrimidines I (R = 4-ClC6H4, Ph; R1 = Et, H Me, Ph) in protic solvents led to the formation of the new 4-amino-1,3,5-triazin-2-yl ketones II in high yields. The structures of II were elucidated by spectroscopic means, especially by 13C-NMR and UV data. Photooxygenation of I (R = 4-ClC6H4, R1 = Et) under reductive conditions, e.g. in the presence of excess of NaBH4, gave 5,6-dihydro-5-hydroxy-4(3H)-pyrimidinone III, the structure of which was determined by x-ray anal. In the proposed mechanisms for both types of reactions, a dipolar ion formed by attack of 1O2 on C5 is assumed to be a common intermediate. For the new efficient synthesis of 1,3,5-triazines from 2,4-diaminopyrimidines, a 5-aryl substituent seems to be essential. In the experiment, the researchers used many compounds, for example, Ethyl 2,4-diaminopyrimidine-5-carboxylate(cas: 15400-54-1Related Products of 15400-54-1)

Ethyl 2,4-diaminopyrimidine-5-carboxylate(cas: 15400-54-1) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Related Products of 15400-54-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Zhang, Ji-Quan; Luo, Yong-Jie; Xiong, Yan-Shi; Yu, Yang; Tu, Zheng-Chao; Long, Zi-Jie; Lai, Xiao-Ju; Chen, Hui-Xuan; Luo, Yu; Weng, Jiang; Lu, Gui published 《Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors》.Journal of Medicinal Chemistry published the findings.HPLC of Formula: 3764-01-0 The information in the text is summarized as follows:

Three series of substituted pyrimidines were designed and synthesized. All target compounds were screened for kinase inhibitory activities against PI3Kα, and most IC50 values were found within the nanomolar range. Compounds 5d and 5p displayed comparable activities relative to the pos. control 5a. P also showed a significant isoenzyme selectivity (PI3Kβ/α). Also, the cytotoxicities of these pyrimidines against human cancer cell lines were evaluated and the in vivo anticancer effect of 5d was also tested. The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0HPLC of Formula: 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.HPLC of Formula: 3764-01-0

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Liang, Xuewu; Zang, Jie; Zhu, Mengyuan; Gao, Qianwen; Wang, Binghe; Xu, Wenfang; Zhang, Yingjie published 《Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1H)-pyrazole Derivatives as JAKs Inhibitors》.ACS 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:

Abnormalities in the JAK/STAT signaling pathway lead to many diseases such as immunodeficiency, inflammation, and cancer. Herein, we designed and synthesized a series of 4-amino-(1H)-pyrazole derivatives as potent JAKs inhibitors for cancer treatment. Results from in vitro protein kinase inhibition experiments indicated that some compounds are potent JAKs inhibitors. For example, the IC50 values of compound I against JAK1, JAK2, and JAK3 were 3.4, 2.2, and 3.5 nM, resp. In cell culture experiments, compound I showed potent antiproliferative activity against various cell lines (PC-3, HEL, K562, MCF-7, and MOLT4) at low micromolar levels, while compound II showed selective cytotoxicity at submicromolar levels against HEL (IC50: 0.35 μM) and K562 (IC50: 0.37 μM) cell lines. It is worth noting that both I and II showed more potent antiproliferative activities than the approved JAKs inhibitor Ruxolitinib. 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

In 2018,Chen, Dizhong; Soh, Chang Kai; Goh, Wei Huang; Wang, Haishan published 《Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma》.Journal of Medicinal Chemistry published the findings.Electric Literature of C6H3Cl2N3 The information in the text is summarized as follows:

Class I histone deacetylases (HDACs) are highly expressed and/or upregulated in hepatocellular carcinoma (HCC) and are associated with aggressiveness, spread, and increased mortality of HCC. Activation of phosphatidylinositol 3-kinase-Akt-mammalian target of rapamycin (PI3K/Akt/mTOR) signaling pathway was involved in the development of HCC and acquired resistance to sorafenib. A series of purine or 5H-pyrrolo[3,2-d]pyrimidine based hydroxamates were designed and developed as multitarget drugs to modulate both HDACs and the PI3K/Akt/mTOR pathway. Among 39 cell lines screened, the mols. (e.g., I, II, and III) were the most selective against leukemia, lymphoma, and HCC cells; they also demonstrated target modulation in cancer cell lines and in mice bearing MV4-11 and HepG2 tumors. Compound II in particular showed significant single agent oral efficacy in hypervascular liver cancer models (e.g., HepG2, HuH-7, and Hep3B) and was well-tolerated. These encouraging results, along with its favorable target profile and tissue distribution, warrant further development of II. The experimental process involved the reaction of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Electric Literature of C6H3Cl2N3)

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. Electric Literature of C6H3Cl2N3They 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

In 2018,Journal of Medicinal Chemistry included an article by Rageot, Denise; Bohnacker, Thomas; Melone, Anna; Langlois, Jean-Baptiste; Borsari, Chiara; Hillmann, Petra; Sele, Alexander M.; Beaufils, Florent; Zvelebil, Marketa; Hebeisen, Paul; Loscher, Wolfgang; Burke, John; Fabbro, Doriano; Wymann, Matthias P.. Name: 2,4,6-Trichloropyrimidine. The article was titled 《Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders》. The information in the text is summarized as follows:

Mechanistic target of rapamycin (mTOR) promotes cell proliferation, growth, and survival and is overactivated in many tumors and central nervous system disorders. I is a novel, potent, selective, and brain penetrable inhibitor of mTORC1/2 kinase. I showed excellent selectivity for mTOR over PI3K and protein kinases and efficiently prevented cancer cell growth in a 66 cancer cell line panel. In C57BL/6J and Sprague-Dawley mice, maximum concentration (Cmax) in plasma and brain was reached after 30 min, with a half-life (t1/2) > 5 h. In an ovarian carcinoma mouse xenograft model (OVCAR-3), daily dosing of I inhibited tumor growth significantly. Moreover, I attenuated epileptic seizures in a tuberous sclerosis complex (TSC) mouse model. In conclusion, I inhibits mTOR kinase potently and selectively, shows antitumor effects in vitro and in vivo, and promises advantages in CNS indications due to its brain/plasma distribution ratio. The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Name: 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.Name: 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia