Category: pyrimidines

HPLC of Formula: 213743-31-8On May 17, 2013 ,《Chemical Interrogation of the Neuronal Kinome Using a Primary Cell-Based Screening Assay》 appeared in ACS Chemical Biology. The author of the article were Al-Ali, Hassan; Schurer, Stephan C.; Lemmon, Vance P.; Bixby, John L.. The article conveys some information:

A fundamental impediment to functional recovery from spinal cord injury (SCI) and traumatic brain injury is the lack of sufficient axonal regeneration in the adult central nervous system. There is thus a need to develop agents that can stimulate axon growth to re-establish severed connections. Given the critical role played by protein kinases in regulating axon growth and the potential for pharmacol. intervention, small mol. protein kinase inhibitors present a promising therapeutic strategy. Here, the authors report a robust cell-based phenotypic assay, utilizing primary rat hippocampal neurons, for identifying small mol. kinase inhibitors that promote neurite growth. The assay is highly reliable and suitable for medium-throughput screening, as indicated by its Z’-factor of 0.73. A focused structurally diverse library of protein kinase inhibitors was screened, revealing several compound groups with the ability to strongly and consistently promote neurite growth. The best performing bioassay hit robustly and consistently promoted axon growth in a postnatal cortical slice culture assay. This study can serve as a jumping-off point for structure activity relationship (SAR) and other drug discovery approaches toward the development of drugs for treating SCI and related neurol. pathologies. In the part of experimental materials, we found many familiar compounds, such as 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8HPLC of Formula: 213743-31-8)

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) 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. HPLC of Formula: 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Category: pyrimidinesOn October 15, 2010 ,《One-Pot Etherification of Purine Nucleosides and Pyrimidines》 was published in Organic Letters. The article was written by Kokatla, Hari Prasad; Lakshman, Mahesh K.. The article contains the following contents:

A one-pot synthesis of ethers derived from inosine, guanosine, 2′-deoxyguanosine, and pyrimidinones is described. Exposure of the heterocycle to 1H-benzotriazol-1-yl-oxy-tris(dimethylamino)phosphonium hexafluorophosphate (BOP) and Cs2CO3 produces a reactive intermediate, which is converted to the desired ether by subsequent addition of an appropriate alc. or phenol and Cs2CO3. Although rapid formation of HMPA from BOP can occur in the presence of an alc. and base, as demonstrated by the reaction with methanol, under appropriate conditions these heteroaryl ethers can be efficiently synthesized. After reading the article, we found that the author used 2-Methoxy-4-methylpyrimidine(cas: 14001-60-6Category: pyrimidines)

2-Methoxy-4-methylpyrimidine(cas: 14001-60-6) is a member of ether. Friedel Crafts reaction, for example, adds an alkyl or acyl group to aromatic ethers when they react with an alkyl or acyl halide in the presence of a Lewis acid as a catalyst.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Pyrimidine synthesis from ethyl ethoxymethylenecyanoacetate and amidines》 was published in Tetrahedron Letters in 1969. These research results belong to Nishigaki, Sadao; Aida, Kyoko; Senga, Keitaro; Yoneda, Fumio. Synthetic Route of C7H10N4O2 The article mentions the following:

Treatment of 1 equivalent EtOH:C(CN)CO2Et(I) with 3 equivalents MeC(:NH)NH2 (II) in cold EtOH and maintaining the mixture at 0° 18 hrs. yielded 85.5% 5-cyano-4-hydroxy-2-methylpyrimidine acetamidinate (III, R = Me) (IV), m. 184-8° (EtOAc). Use of 2 or 1 equivalent II decreased the yields of IV to 69.0 and 20.3%, resp. A small amount of ethyl 4-amino-2-methyl-5-pyrimidinecarboxylate (V) was extracted from the reactions mixtures with Et2O. IV neutralized with AcOH gave 5-cyano-4-hydroxy-2-methylpyrimidine, reconverted to IV by treating with an equimolar amount of II in alc. The mass spectrum of IV revealed the strong parent ions m/e 135, 58 but no mol. ion, m/e 193, corresponding to N-(3-acetamidino-2-cyanoacryloyl)acetamidine, H2NCR:NCH:C(CN)CONHCR:-NH (VI, R = Me) (VII). The reactions of I with 2-ethyl-2-thiopseudourea (VIII) in MeOH readily gave Et 3-[[amino-(ethylthio)methylene]amino]-2-cyanoacrylate (IX); III (R = EtS) (X), m. 175-7°; and traces of V. Increase of the ratio of VIII to I from 1:1 to 4:1 led to decrease of the % yield of IX and increase of X. The reactions of guanidine with I in cold alc. gave predominantly Et 2,4-diamino-5-pyrimidinecarboxylate (XI), m. 215-17° (alc.), along with a trace of III (R = NH2) (XII), m. >300° (MeOH), converted to 2-amino-5-cyano-4-hydroxypyrimidine, m. >300° (AcOH), by treating with AcOH. Use of a large excess of guanidine increased the yield of XI to 95% in the absence of XII. After reading the article, we found that the author used Ethyl 2,4-diaminopyrimidine-5-carboxylate(cas: 15400-54-1Synthetic Route of C7H10N4O2)

Ethyl 2,4-diaminopyrimidine-5-carboxylate(cas: 15400-54-1) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Synthetic Route of C7H10N4O2

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Product class 12: pyrimidines》 was written by von Angerer, S.. Recommanded Product: 2-Methoxy-4-methylpyrimidine And the article was included in Science of Synthesis in 2004. The article conveys some information:

A review. Methods for preparing pyrimidines are reviewed including cyclization, ring transformation, aromatization and substituent modification. After reading the article, we found that the author used 2-Methoxy-4-methylpyrimidine(cas: 14001-60-6Recommanded Product: 2-Methoxy-4-methylpyrimidine)

2-Methoxy-4-methylpyrimidine(cas: 14001-60-6) 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.Recommanded Product: 2-Methoxy-4-methylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Design, synthesis and antibacterial activities of triazole-pyrimidine derivatives as SecA inhibitors》 was written by Bamba, Fante; Etienne, Camara Tchambaga; Siomenan, Coulibali; Jacques, Akpa Sagne; Souleymane, Coulibaly; Ane, Adjou. Recommanded Product: 3764-01-0This research focused ontriazole pyrimidine preparation antibacterial activity. The article conveys some information:

Background: To highlight the magnitude of the important challenge now facing scientists, drug resistance needs exploration of novel antimicrobial agents. The identification of new and vital target in bacteria and then designing their inhibitors can be explored. Thus, targeting SecA, a central component of the bacterial general secretion system, is a promising strategy for the development of novel antimicrobials. Objective: To evaluate new compounds as SecA inhibitors synthesized by structural modification of bistriazole SCA-21. Method: A new compounds were synthesized and evaluated for antibacterial activity against Escherichia coli NR698 (E. coli a leaky mutant), Staphylococcus aureus (S. aureus) and Bacillus anthracis (B. anthracis). Results: Some novel triazole-pyrimidine derivatives by structural modification of known SecA inhibitor SCA 21 were synthesized and their structures were confirmed by 1H NMR, 13C NMR and Mass spectral anal. The synthesized compound showed antimicrobial activity against E. coli NR698 (a leaky mutant), S. aureus and B. anthracis Sterne. Conclusion: Five novel triazole-pyrimidine derivatives were designed, synthesized and evaluated as SecA inhibitors. At the end of this study, compound SCA 259 with azide pentyl group was found as the most potent inhibitor. It expressed better inhibitory activity against SecA ATPase than else known inhibitor SCA 21. The experimental part of the paper was very detailed, including the reaction process of 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 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.Recommanded Product: 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

AlNeyadi, Shaikha S.; Adem, Abdu; Amer, Naheed; Ghattas, Mohammad A.; Atatreh, Noor; Salem, Alaa A.; Abdou, Ibrahim M. published their research in Results in Chemistry in 2021. The article was titled 《Activation of the GLP-1 receptor by chloropyrimidine derivatives》.COA of Formula: C4H2Cl2N2 The article contains the following contents:

The anti-diabetic activities of a series of chloropyrimidine derviativeswere investigated after they were designed, synthesized, and docked against the GLP-1 receptor target. In comparison to exenatide, which was utilized as a reference drug, the three chloropyrimidine synthesized compounds I, II and III exhibited potent in vitro and in vivo antidiabetic activities. Interestingly, compounds I, II and III showed to be the most effective in lowering blood glucose levels and led to even higher glucose uptake than the reference drug, exenatide. Consistent with the in vitro and in vivo data, compounds II and III had the lowest docking energy scores (Glide-XP score = 5.1 kcal/mol) and the greatest ligand efficiency score (> – 0.40 kcal/mol) among all docked compounds These findings give up new possibilities for the development of high-efficacy compounds to treat hyperglycemia. The experimental process involved the reaction of 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

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,Andrs, Martin; Pospisilova, Monika; Seifrtova, Martina; Havelek, Radim; Tichy, Ales; Vejrychova, Katerina; Polednikova, Michaela; Gorecki, Lukas; Jun, Daniel; Korabecny, Jan; Rezacova, Martina published 《Purin-6-one and pyrrolo[2,3-d]pyrimidin-4-one derivatives as potentiating agents of doxorubicin cytotoxicity》.Future Medicinal Chemistry published the findings.Category: pyrimidines The information in the text is summarized as follows:

Aim: DNA damage response plays an eminent role in patients′ response to conventional chemotherapy and radiotherapy. Its inhibition is of great interest as it can overcome cancer cell resistance and reduce the EDs of DNA damaging agents. Results & methodol.: We have focused our research on phosphatidylinositol 3-kinase-related kinases and prepared 35 novel compounds through a scaffold hopping approach. The newly synthesized inhibitors were tested on a panel of nine cancer and one healthy cell lines alone and in combination with appropriate doses of doxorubicin. Conclusion: Five novel compounds 4f, 10b, 15g, 7e and 15f in combination with doxorubicin showed significant antiproliferative effect on seven cancer cell lines while not affecting the cell growth alone. In the experiment, the researchers used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Category: pyrimidines)

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. 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.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2017,Kamijo, Shin; Kamijo, Kaori; Murafuji, Toshihiro published 《Synthesis of Alkylated Pyrimidines via Photoinduced Coupling Using Benzophenone as a Mediator》.Journal of Organic Chemistry published the findings.Formula: C4HCl3N2 The information in the text is summarized as follows:

Alkylated pyrimidines such as I (R = Cl, MeO) were prepared regioselectively by photochem. coupling of cyclic ethers, carbamates, γ-butyrolactam, and tetrahydrothiophene (THT) with methanesulfonylpyrimidines such as II (R = Cl, MeO) using benzophenone as the sole photochem. mediator. The heterocyclic substituents were selectively introduced at the nonacidic C(sp3)-H bond proximal to their heteroatoms, and at the methanesulfonyl-substituted position of the pyrimidines. This method was used to prepare an analog of the Aurora kinase inhibitor MK-0457. The experimental process involved the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Formula: C4HCl3N2)

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.Formula: C4HCl3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2014,Su, Qibin; Ioannidis, Stephanos; Chuaqui, Claudio; Almeida, Lynsie; Alimzhanov, Marat; Bebernitz, Geraldine; Bell, Kirsten; Block, Michael; Howard, Tina; Huang, Shan; Huszar, Dennis; Read, Jon A.; Rivard Costa, Caroline; Shi, Jie; Su, Mei; Ye, Minwei; Zinda, Michael published 《Discovery of 1-Methyl-1H-imidazole Derivatives as Potent Jak2 Inhibitors》.Journal of Medicinal Chemistry published the findings.Synthetic Route of C6H3Cl2N3 The information in the text is summarized as follows:

Structure based design, synthesis, and biol. evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clin. candidate AZD1480 (I), optimization of the series led to the discovery of compound II, a potent, orally bioavailable Jak2 inhibitor. Compound II displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound II demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Synthetic Route of C6H3Cl2N3)

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. Synthetic Route of C6H3Cl2N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2010,Tumkevicius, Sigitas; Dodonova, Jelena; Kazlauskas, Karolis; Masevicius, Viktoras; Skardziute, Lina; Jursenas, Saulius published 《Synthesis and photophysical properties of oligoarylenes with a pyrrolo[2,3-d]pyrimidine core》.Tetrahedron Letters published the findings.Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

The Pd-catalyzed Suzuki-Miyaura reaction of 2,4-dichloropyrrolo[2,3-d]pyrimidine with arylboronates was studied. Pd(OAc)2/dicyclohexyl(2-biphenyl)phosphine/K3PO4 was an efficient catalyst system to prepare 4-aryl-2-chloro- and 2,4-diarylpyrrolo[2,3-d]pyrimidines. Novel non-linear mols. consisting of a pyrrolo[2,3-d]pyrimidine core and aryl branches were elucidated as blue light-emitters with fluorescence quantum yields of 4-67% in THF solution The impact of an electron-withdrawing CO2CMe3 group attached to the pyrrole ring of pyrrolopyrimidines on optical properties is discussed. 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: 90213-66-4Recommanded Product: 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. 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. Recommanded Product: 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia