Tag: 100-200

Pyrimidines. XLII. Synthesis of 2- and 6-substituted 4-fluoropyrimidines was written by Shkurko, O. P.;Baram, S. G.;Mamaev, V. P.. And the article was included in Izvestiya Sibirskogo Otdeleniya Akademii Nauk SSSR, Seriya Khimicheskikh Nauk in 1973.Reference of 51421-99-9 This article mentions the following:

4-Fluoropyrimidines I (R = H, Me Ph, OMe, CF3, F, NMe2, R1 = Me, H, Ph, F, MeO, NH2, NMe2) were prepared in 10-97% yields by fluorination of the corresponding chloropyrimidines by CsF in DMF or methylpyrrolidone and by nucleophilic substitution of a F atom in difluoro- and trifluoro- pyrimidines. In the experiment, the researchers used many compounds, for example, 4-Chloro-2-methoxypyrimidine (cas: 51421-99-9Reference of 51421-99-9).

4-Chloro-2-methoxypyrimidine (cas: 51421-99-9) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Reference of 51421-99-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor was written by Borsari, Chiara;Rageot, Denise;Dall’Asen, Alix;Bohnacker, Thomas;Melone, Anna;Sele, Alexander M.;Jackson, Eileen;Langlois, Jean-Baptiste;Beaufils, Florent;Hebeisen, Paul;Fabbro, Doriano;Hillmann, Petra;Wymann, Matthias P.. And the article was included in Journal of Medicinal Chemistry in 2019.Name: 4-Dimethoxymethylpyrimidin-2-ylamine This article mentions the following:

The mechanistic target of rapamycin (mTOR) plays a pivotal role in growth and tumor progression and is an attractive target for cancer treatment. ATP-competitive mTOR kinase inhibitors (TORKi) have the potential to overcome limitations of rapamycin derivatives in a wide range of malignancies. Herein, we exploit a conformational restriction approach to explore a novel chem. space for the generation of TORKi. Structure-activity relationship (SAR) studies led to the identification of compound 12b with a ∼450-fold selectivity for mTOR over class I PI3K isoforms. Pharmacokinetic studies in male Sprague Dawley rats highlighted a good exposure after oral dosing and a min. brain penetration. CYP450 reactive phenotyping pointed out the high metabolic stability of 12b. These results identify the tricyclic pyrimido-pyrrolo-oxazine moiety as a novel scaffold for the development of highly selective mTOR inhibitors for cancer treatment. In the experiment, the researchers used many compounds, for example, 4-Dimethoxymethylpyrimidin-2-ylamine (cas: 165807-05-6Name: 4-Dimethoxymethylpyrimidin-2-ylamine).

4-Dimethoxymethylpyrimidin-2-ylamine (cas: 165807-05-6) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Name: 4-Dimethoxymethylpyrimidin-2-ylamine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Tetrahydro-3H-pyrazolo[4,3-a]phenanthridine-based CDK inhibitor was written by Opoku-Temeng, Clement;Dayal, Neetu;Hernandez, Delmis E.;Naganna, N.;Sintim, Herman O.. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2018.Quality Control of 2-Methoxypyrimidine-5-carbaldehyde This article mentions the following:

Cyclin-dependent kinases have emerged as important targets for cancer therapy. HSD992, containing a novel scaffold based on the tetrahydro-3H-pyrazolo[4,3-a]phenanthridine core, inhibits CDK2/3 but not other CDKs and also potently inhibits several cancer cell lines. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Quality Control of 2-Methoxypyrimidine-5-carbaldehyde).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Quality Control of 2-Methoxypyrimidine-5-carbaldehyde

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The coloration reaction mechanism of 6-aminouracil derivatives with Ehrlich reagent and its application to the colorimetric determination method. II was written by Nakashima, Kenichiro. And the article was included in Yakugaku Zasshi in 1977.Product Details of 54030-56-7 This article mentions the following:

6-Amino-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine (I) [1004-40-6] and its N- or S-substituted derivatives are hydrolyzed by p-toluenesulfonic acid or HCl to the corresponding barbiturates. These barbiturates condense with the Ehrlich reagent [100-10-7] in the presence of an acid catalyst to afford stable benzylidene compounds These reactions were found to be almost quant. The optimal exptl. conditions were also established for using the above reactions for the quant. colorimetric determination of I derivatives In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Product Details of 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Product Details of 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Dual Inhibitors of 8-Oxoguanine Surveillance by OGG1 and NUDT1 was written by Tahara, Yu-ki;Kietrys, Anna M.;Hebenbrock, Marian;Lee, Yujeong;Wilson, David L.;Kool, Eric T.. And the article was included in ACS Chemical Biology in 2019.Product Details of 20090-58-8 This article mentions the following:

Oxidative damage in DNA is one of the primary sources of mutations in the cell. The activities of repair enzymes 8-oxoguanine DNA glycosylase (OGG1) and human MutT Homolog 1 (NUDT1 or MTH1), which work together to ameliorate this damage, are closely linked to mutagenesis, genotoxicity, cancer, and inflammation. Here we have undertaken the development of small-mol. dual inhibitors of the two enzymes as tools to test the relationships between these pathways and disease. The compounds preserve key structural elements of known inhibitors of the two enzymes, and they were synthesized and assayed with recently developed luminescence assays of the enzymes. Further structural refinement of initial lead mols. yielded compound 5 (I) (SU0383) with IC50 (NUDT1) = 0.034μM, IC50 (OGG1) = 0.49μM. I displayed low toxicity in two human cell lines at 10μM. Experiments confirm the ability of I to increase sensitivity of tumor cells to oxidative stress. Dual inhibitors of these two enzymes are expected to be useful in testing multiple hypotheses regarding the roles of 8-oxo-dG in multiple disease states. In the experiment, the researchers used many compounds, for example, 4-Chloro-5-methylpyrimidin-2-amine (cas: 20090-58-8Product Details of 20090-58-8).

4-Chloro-5-methylpyrimidin-2-amine (cas: 20090-58-8) belongs to pyrimidine derivatives. The aromatic compound pyrimidine, and its derivatives, are ubiquitous in nature. They are found in nucleic acids, vitamins, amino acids, antibiotics, alkaloids, and a variety of toxins. Pyrimidine derivatives 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.Product Details of 20090-58-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Detection of active groups in alkylpyrimidines. Study of the mobility of hydrogen by hydrogen-deuterium isotope exchange. I. Qualitative kinetics was written by Dizabo, Pierre;Monier, Jean C.;Pompon, Alain. And the article was included in Journal of Labelled Compounds in 1971.Electric Literature of C6H9N3 This article mentions the following:

Me groups bound to heterocyclic rings exchange H for D. This exchange is studied for alkyl or aminoalkylpyrimidines in acid. The qual. results obtained as a function of acidity, substituent location, and temperature confirm the reaction mechanism proposed by Brown except in the case of 2-amino-4,6-dimethylpyrimidine. In the experiment, the researchers used many compounds, for example, 4,5-Dimethylpyrimidin-2-amine (cas: 1193-74-4Electric Literature of C6H9N3).

4,5-Dimethylpyrimidin-2-amine (cas: 1193-74-4) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. For example, the neurotoxin tetrodotoxin is a pyrimidine derivative. It is found in a number of species including the Japanese puffer fish, the blue-ringed octopus, and the orange-bellied newt. Tetrodotoxin prevents the transmission of nerve signals and can result in paralysis and death.Electric Literature of C6H9N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Efficient coupling of 2-halopyrimidines to 2,2′-bipyrimidines was written by Nasielski, J.;Standaert, A.;Nasielski-Hinkens, R.. And the article was included in Synthetic Communications in 1991.Recommanded Product: 2-Bromo-4,6-dimethylpyrimidine This article mentions the following:

Pyrimidines I (R = H, Me, Ph; R¹ = Br, Cl) have been dimerized to the corresponding 2,2′-bipyrimidines in good yields by Tiecco’s method using NiCl₂, PPh₃ and Zn in DMF. In the experiment, the researchers used many compounds, for example, 2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3Recommanded Product: 2-Bromo-4,6-dimethylpyrimidine).

2-Bromo-4,6-dimethylpyrimidine (cas: 16879-39-3) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Recommanded Product: 2-Bromo-4,6-dimethylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Solvent-free microwave multicomponent regiospecific synthesis of pyrimido[4,5-c]isoquinolines and evaluation in vitro of their antifungal properties was written by Quiroga, Jairo;Cisneros, Carlos;Insuasty, Braulio;Abonia, Rodrigo;Nogueras, Manuel;Sortino, Maximiliano;Zacchino, Susana. And the article was included in Journal of Heterocyclic Chemistry in 2006.Recommanded Product: 54030-56-7 This article mentions the following:

The solvent-free multicomponent reaction of 6-aminopyrimidin-4(3H)-ones with dimedone and N,N-dimethylformamide dimethylacetal under microwave irradiation yields pyrimido[4,5-c]isoquinolinones. In this process, the intermediate of cyclization was isolated. The structure of the synthesized compounds was determined on the basis of NMR measurements, especially by ¹H,¹H-, ¹H ,¹³C COSY, and DEPT. These compounds showed antifungal in vitro activity particularly against dermatophytes. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Recommanded Product: 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Recommanded Product: 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reactions of 6-aminopyrimidin-4(3H)-ones with electron-deficient alkenyl derivatives. Easy preparation of heterocyclic analogs of sangivamycin was written by Cobo, Justo;Sanchez, Adolfo;Nogueras, Manuel. And the article was included in Tetrahedron in 1998.Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one This article mentions the following:

Aminopyrimidinones I (R = H, Me; X = C(OMe):N, C(SMe):N) and uracils I (R = H, Me; X = CONH, CONMe) react with maleic anhydride to give pyrrolopyrimidines II. I (R = H, Me; X = C(OMe):N, C(SMe):N) undergo Michael addition with maleimide to give stable maleimides III (R = H, Me; X = C(OMe):N, C(SMe):N). I (R = Me, X = C(SMe):N) also undergoes a Diels-Alder reaction with maleimide to give 13% of pyrrolopyrimidine IV. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.Name: 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Diastereoselective Trifluoroacetylation of Highly Substituted Pyrrolidines by a Dakin-West Process was written by Baumann, Marcus;Baxendale, Ian R.. And the article was included in Journal of Organic Chemistry in 2016.Safety of 2-Methoxypyrimidine-5-carbaldehyde This article mentions the following:

A robust approach allowing for the efficient trifluoroacetylation of a series of highly substituted pyrrolidines in a diastereoselective manner is reported. The transformation is based on a Dakin-West reaction of advanced pyrrolidine 2-carboxylic acid derivatives that can be assembled stereoselectively in four synthetic steps. Importantly, this work demonstrates how the introduction of lateral substituents on the pyrrolidine scaffold enables the generation of the desired trifluoroacetylation products, which was not possible previously due to the exclusive formation of trifluoromethylated oxazoles. In the course of this work we succeeded for the first time in isolating and characterizing (HRMS, IR, ¹H, ¹³C and ¹⁹F NMR, X-ray) different intermediates of the Dakin-West reaction allowing us to probe its mechanism. In the experiment, the researchers used many compounds, for example, 2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1Safety of 2-Methoxypyrimidine-5-carbaldehyde).

2-Methoxypyrimidine-5-carbaldehyde (cas: 90905-32-1) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Safety of 2-Methoxypyrimidine-5-carbaldehyde

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia