Day: October 14, 2022

Application of 213743-31-8On October 2, 2000 ,《Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Arnold, L. D.; Calderwood, D. J.; Dixon, R. W.; Johnston, D. N.; Kamens, J. S.; Munschauer, R.; Rafferty, P.; Ratnofsky, S. E.. The article contains the following contents:

Pyrrolo[2,3-d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of lck in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Application of 213743-31-8)

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. Application of 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylateOn October 8, 2009 ,《RNase H Active Site Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase: Design, Biochemical Activity, and Structural Information》 was published in Journal of Medicinal Chemistry. The article was written by Kirschberg, Thorsten A.; Balakrishnan, Mini; Squires, Neil H.; Barnes, Tiffany; Brendza, Katherine M.; Chen, Xiaowu; Eisenberg, Eugene J.; Jin, Weili; Kutty, Nilima; Leavitt, Stephanie; Liclican, Albert; Liu, Qi; Liu, Xiaohong; Mak, John; Perry, Jason K.; Wang, Michael; Watkins, William J.; Lansdon, Eric B.. The article contains the following contents:

Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function. These mols. can coordinate to two divalent metal ions in the RNase H active site. Inhibition of enzymic activity was measured in a biochem. assay, but no antiviral effect was observed Binding was demonstrated via a solid state structure of the isolated p15-Ec domain of HIV-1 RT showing inhibitor and two Mn(II) ions bound to the RNase H active site. The experimental part of the paper was very detailed, including the reaction process of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate(cas: 519032-07-6Application In Synthesis of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylate)

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. Application In Synthesis of Methyl 2-benzyl-5,6-dihydroxypyrimidine-4-carboxylateThey 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

Category: pyrimidinesOn September 18, 2020 ,《Development of a Scalable Route for a Highly Polar Heterocyclic Aminocyclopropyl Building Block》 was published in Organic Process Research & Development. The article was written by Schafer, Gabriel; Ahmetovic, Muhamed; Fleischer, Tony; Abele, Stefan. The article contains the following contents:

A robust and scalable route toward key heterocyclic building block 1-(pyrimidin-2-yl)cyclopropan-1-amine hydrochloride from cyclopropanated starting material 1-amino-1-cyclopropanecarbonitrile hydrochloride was successfully developed. The key to success was the construction of a pyrimidine ring via cyclization from an amidine intermediate and a bench-stable 2-chloro vinamidinium hexafluorophosphate salt. The cyclization was performed under mild conditions, and the resulting 4-chloropyrimidine derivative was isolated in high yield and purity. The final hydrogenation was intensively optimized: A combination of Pd(OH)2/C as a catalyst and NaOMe as a base at 1 bar H2 pressure in MeOH simultaneously cleaved the Cbz group and dechlorinated the pyrimidine ring while at the same time suppressing the over-reduction of the pyrimidine ring to below 1.0%. After acidification with HCl, followed by removal of the catalyst and NaCl by filtration, the final product was isolated in high yield and purity as a bench-stable off-white solid. The overall yield of the five-step sequence was 57%. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3Category: pyrimidines)

Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3) 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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ham, Won Seok; Choi, Hoonchul; Zhang, Jianbo; Kim, Dongwook; Chang, Sukbok published an article on February 23 ,2022. The article was titled 《C2-Selective, Functional-Group-Divergent Amination of Pyrimidines by Enthalpy-Controlled Nucleophilic Functionalization》, and you may find the article in Journal of the American Chemical Society.Reference of 5-Bromo-4-ethylpyrimidine The information in the text is summarized as follows:

A synthetic platform for site-selective C-H functionalization that affords pyrimidinyl iminium salt intermediates, which then can be transformed into various amine products I (R = azanyl, 5-(trifluoromethyl)-1,2,3,4-tetrahydropyridin-1-yl, methylaminyl, etc.; R1 = H, Ph) in situ. was described. Mechanism-based reagent design allowed for the C2-selective amination of pyrimidines II, opening the new scope of site-selective heteroaryl C-H functionalization. This method is compatible with a broad range of pyrimidines II with sensitive functional groups, and can access complex aminopyrimidines I in high selectivity. The experimental part of the paper was very detailed, including the reaction process of 5-Bromo-4-ethylpyrimidine(cas: 951884-36-9Reference of 5-Bromo-4-ethylpyrimidine)

5-Bromo-4-ethylpyrimidine(cas: 951884-36-9) 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.Reference of 5-Bromo-4-ethylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Lim, Sang Min; Xie, Ting; Westover, Kenneth D.; Ficarro, Scott B.; Tae, Hyun Seop; Gurbani, Deepak; Sim, Taebo; Marto, Jarrod A.; Janne, Pasi A.; Crews, Craig M.; Gray, Nathanael S. published their research in Bioorganic & Medicinal Chemistry Letters on August 15 ,2015. The article was titled 《Development of small molecules targeting the pseudokinase Her3》.Related Products of 213743-31-8 The article contains the following contents:

Her3 is a member of the human epidermal growth factor receptor (EGFR) tyrosine kinase family, and it is often either overexpressed or deregulated in many types of human cancer. Her3 has not been the subject of small-mol. inhibitor development because it is a pseudokinase and does not possess appreciable kinase activity. We recently reported on the development of the first selective irreversible Her3 ligand (TX1-85-1) that forms a covalent bond with cysteine 721 which is unique to Her3 among all kinases. We also developed a bi-functional compound (TX2-121-1) containing a hydrophobic adamantane moiety and the same warhead of TX1-85-1 that is capable of inhibiting Her3-dependent signaling and growth. Here we report on the structure-based medicinal chem. effort that resulted in the discovery of these two compounds7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Related Products of 213743-31-8) was used in this study.

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.Related Products of 213743-31-8

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reddy, Bhoomireddy Rajendra Prasad; Reddy, Motakatla Venkata Krishna; Reddy, Peddiahgari Vasu Govardhana; Kumar, Dharani Praveen; Shankar, Muthukonda V. published an article on February 10 ,2016. The article was titled 《Protonated trititanate nanotubes: an efficient catalyst for one-pot three-component coupling of benzothiazole amines, heterocyclic aldehydes, and dialkyl/diaryl phosphites with a greener perspective》, and you may find the article in Tetrahedron Letters.Product Details of 640769-70-6 The information in the text is summarized as follows:

Nano-size catalysts of TiO2, ZnO, CuO, and protonated trititanate nanotubes (H2Ti3O7) have been investigated for the one-pot three component synthesis of novel α-aminophosphonates from benzothiazole amines, heteroaldehydes, and dialkyl/diaryl phosphites via Kabachnik-Fields reaction. This methodol. provides a new and convenient approach to multicomponent reaction and the H2Ti3O7 nanotubes catalyst is recyclable up to seven cycles. The experimental process involved the reaction of 3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6Product Details of 640769-70-6)

3-(Pyrimidin-5-yl)benzaldehyde(cas: 640769-70-6) 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 640769-70-6

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2017,Leitch, Jamie A.; McMullin, Claire L.; Paterson, Andrew J.; Mahon, Mary F.; Bhonoah, Yunas; Frost, Christopher G. published 《Ruthenium-Catalyzed para-Selective C-H Alkylation of Aniline Derivatives》.Angewandte Chemie, International Edition published the findings.Safety of 2,4,6-Trichloropyrimidine The information in the text is summarized as follows:

The para-selective C-H alkylation of aniline derivatives furnished with a pyrimidine auxiliary is herein reported. This reaction is proposed to take place via an N-H-activated cyclometalate formed in situ. Exptl. and DFT mechanistic studies elucidate a dual role of the ruthenium catalyst. Here the ruthenium catalyst can undergo cyclometalation by N-H metalation (as opposed to C-H metalation in meta-selective processes) and form a redox active ruthenium species, to enable site-selective radical addition at the para position. The results came from multiple reactions, including the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Safety of 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.Safety of 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2019,Beilstein Journal of Organic Chemistry included an article by Sisulins, Andrejs; Bucevieius, Jonas; Tseng, Yu-Ting; Novosjolova, Irina; Traskovskis, Kaspars; Bizdena, Erika; Chang, Huan-Tsung; Tumkevieius, Sigitas; Turks, Maris. Electric Literature of C6H3Cl2N3. The article was titled 《Synthesis and fluorescent properties of N(9)-alkylated 2-amino-6-triazolylpurines and 7-deazapurines》. The information in the text is summarized as follows:

The synthesis of novel fluorescent N(9)-alkylated 2-amino-6-triazolylpurine and 7-deazapurine derivatives is described. A new C(2)-regioselectivity in the nucleophilic aromatic substitution reactions of 9-alkylated-2,6-diazidopurines and 7-deazapurines with secondary amines has been disclosed. The obtained intermediates, 9-alkylated-2-amino-6-azido-(7-deaza)purines, were transformed into the title compounds by CuAAC reaction. The designed compounds belong to the push-pull systems and possess promising fluorescence properties with quantum yields in the range from 28% to 60% in acetonitrile solution Due to electron-withdrawing properties of purine and 7-deazapurine heterocycles, which were addnl. extended by triazole moieties, the compounds with electron-donating groups showed intramol. charge transfer character (ICT/TICT) of the excited states which was proved by solvatochromic dynamics and supported by DFT calculations In the 7-deazapurine series this led to increased fluorescence quantum yield (74%) in THF solution The compounds exhibit low cytotoxicity and as such are useful for the cell labeling studies in the future. 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: 90213-66-4Electric Literature of C6H3Cl2N3) was used in this study.

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

《A short de novo synthesis of nucleoside analogs》 was written by Meanwell, Michael; Silverman, Steven M.; Lehmann, Johannes; Adluri, Bharanishashank; Wang, Yang; Cohen, Ryan; Campeau, Louis-Charles; Britton, Robert. HPLC of Formula: 1193-21-1 And the article was included in Science (Washington, DC, United States) in 2020. The article conveys some information:

Nucleoside analogs are commonly used in the treatment of cancer and viral infections. Their syntheses benefit from decades of research but are often protracted, unamenable to diversification, and reliant on a limited pool of chiral carbohydrate starting materials. We present a process for rapidly constructing nucleoside analogs from simple achiral materials. Using only proline catalysis, heteroaryl-substituted acetaldehydes are fluorinated and then directly engaged in enantioselective aldol reactions in a one-pot reaction. A subsequent intramol. fluoride displacement reaction provides a functionalized nucleoside analog. The versatility of this process is highlighted in multigram syntheses of D- or L-nucleoside analogs, locked nucleic acids, iminonucleosides, and C2′- and C4′-modified nucleoside analogs. This de novo synthesis creates opportunities for the preparation of diversity libraries and will support efforts in both drug discovery and development. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1HPLC of Formula: 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) 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.HPLC of Formula: 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of 4,6-DichloropyrimidineIn 2019 ,《Design, Synthesis, and Structure-Activity Relationship of New Arylpyrazole Pyrimidine Ether Derivatives as Fungicides》 appeared in Journal of Agricultural and Food Chemistry. The author of the article were Zhang, Pengfei; Guan, Aiying; Xia, Xiaoli; Sun, Xufeng; Wei, Siyuan; Yang, Jinlong; Wang, Junfeng; Li, Zhinian; Lan, Jie; Liu, Changling. The article conveys some information:

To explore a novel fungicide effectively against cucumber downy mildew (CDM), a series of new arylpyrazole containing pyrimidine ether derivatives were designed and synthesized by employing the intermediate derivatization method (IDM). The structures of synthesized compounds were identified by 1H NMR, 13C NMR, elemental analyses, MS, and X-ray diffraction. Bioassays demonstrated that some of the title compounds exhibited excellent fungicidal activities against CDM. Especially, compound I (EC50 = 1.22 mg/L) displayed significantly higher bioactivity than that of com. fungicides diflumetorim and flumorph and nearly equal effect to that of cyazofamid. The relationship between the structure and fungicidal activity of the synthesized compounds was discussed as well. The study showed that compound I was a promising fungicide candidate for further development. In addition to this study using 4,6-Dichloropyrimidine, there are many other studies that have used 4,6-Dichloropyrimidine(cas: 1193-21-1Application In Synthesis of 4,6-Dichloropyrimidine) was used in this study.

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.Application In Synthesis of 4,6-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia