Category: 151266-23-8

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 151266-23-8, name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine. A new synthetic method of this compound is introduced below., Recommanded Product: 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine

87D: Compound 87C (200 mg, 0.77 mmol), ,P0 (488 mg, 2.30 mmol), 4-phenoxybenzene boronic acid (491 mg, 2.32 mmol) and Tetrakis-(triphenylphosphine)palladium (124 mg, 0.1 1 mmol) were dissolved in 2.5 mL of dioxane in a microwave vial. The vial was sealed and the reaction mixture was heated to 180C for 10 min under microwave irradiation. The reaction mixture was partitioned between water and ethylacetate and the organic layer was separated, dried over anhydrous Na2S04, filtered and concentrated. The residue was purified by column chromatography on Si02 using MeOH/CH2C12 (0: 100 to 10:90). Compound 87D was obtained as a white powder (92 mg, 41% yield). NMR (ppm, DMSO): 8.21 (s, 1 H), 7.66 (d, J= 8.8 Hz, 2H), 7.43 (t, J= 7.9 Hz, 2H), 7.21-7.1 1 (m, 5H). LCMS (+esi): 304.2 (M+H+).

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 151266-23-8, 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine.

Reference:
Patent; THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH; LUDWIG INSTITUTE FOR CANCER RESEARCH LIMITED; LESSENE, Guillaume Laurent; BAELL, Jonathan Bayldon; BURGESS, Antony Wilks; MARUTA, Hiroshi; WO2012/3544; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 151266-23-8, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.151266-23-8, name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C5H4IN5, molecular weight is 261.02, as common compound, the synthetic route is as follows.

Compound 2-4 is synthesized as shown in Scheme 2. Compound 1-3 is reacted with isopropyl bromide in dimethylformamide with potassium carbonate at 800C, to provide the 1 -isopropyl pyrazolopyrimidine 2-1. This intermediate with the protected indolyl boronic acid species 2-2, using tetrakistriphenylphosphine palladium catalysis in DME-water solvent at 800C for 4-5 hours, to produce the Suzuki coupling product, compound 2-3. Removal of the protecting groups with acid in dioxane yields the product, 2-( 4-amino-lH-pyrazolo[3,4-d]pyrimidin-3-yl iodide (Cpd. 2-4).

Statistics shows that 151266-23-8 is playing an increasingly important role. we look forward to future research findings about 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine.

Reference:
Patent; INTELLIKINE, INC.; REN, Pingda; LIU, Yi; LI, Liansheng; CHAN, Katrina; WILSON, Troy, Edward; MARTIN, Michael; ROMMEL, Christian; WO2010/6086; (2010); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 151266-23-8, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 151266-23-8, name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine. This compound has unique chemical properties. The synthetic route is as follows.

3-iodo-lH-pyrazolo [3,4-d] pyrimidin-4-amine, respectively, in a 250 mL thick walled reaction flask(1.31 g, 5.0 mmol), (4-phenoxyphenyl) boronic acid (1.28 g, 6.0 mmol), potassium carbonate (1.73 g, 12.5 mmol), 1,4-dioxane (30 mL) and water (6 mL). Pd (dppf) Cl2 (300 mg, 0.41 mmol) was added under nitrogen and the reaction was sealed overnight at 140 C. After completion of the reaction, the reaction mixture was filtered and extracted with dichloromethane 3), washed with saturated brine (60 mL) and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel column chromatography (dichloromethane / methanol (V / V) = 20/1) , 42%).20/1) to give a tint solid (635 mg, 42%

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 151266-23-8, 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine.

Reference:
Patent; Guangdong HEC Pharmaceutical Co., Ltd; LIU, BING; BAI, SHUN; ZHANG, YINGJUN; ZHENG, CHANGCHUN; YANG, TIPING; ZHOU, YOUBAI; (33 pag.)CN105399756; (2016); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 151266-23-8, name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine. This compound has unique chemical properties. The synthetic route is as follows. name: 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine

[00129] To a mixture of 3-iodo-1 H-pyrazolo[3,4-d]pyrimidin-4-amine (1.044 g, 4 mmol), (4-phenoxyphenyl)boronic acid (0.94 g, 4.4 mmol, 1.1 eq), PdCl2(dppf) (0.29 g, 0.4 mmol, 0.1 eq) and Na2CO3 (0.89 g, 8.4 mmol, 2.1 eq) in a 40 ml reaction vial under vacuum, 25 mL of H20/THF (1 :4) is added via a syringe. The mixture is refilled with N2 and heated to 110 C overnight. TLC showed that the reaction is almost completed. Then solvent is evaporated and the residue is suspended in 200 mL (15% THF/EtOAc) and washed with water, brine, dried over Na2SO4, filtered, and evaporated. The residue is purified with a 50 g silica gel cartridge by Combi-flash (0-10% gradient of methanol in DCM to afford 513 mg of 3-(4-phenoxyphenyl)-1 H-pyrazolo[3,4-d]pyrimidin-4-amine. 1HNMR (300 MHz, DMSO-d6): delta 8.22 (s, 1 H), 7.66 (d, 2 H), 7.43 (t, 2 H), 7.10- 7.23 (m, 5 H).

With the rapid development of chemical substances, we look forward to future research findings about 151266-23-8.

Reference:
Patent; BETA PHARMA CANADA INC.; WANG, Zhaoyin; LI, Lianhai; WANG, Zhigang; WO2013/113097; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 151266-23-8, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 151266-23-8 as follows.

Example 13. l-(4-(4-amino-l-cyclopentyl-lH-pyrazolo[3,4-d]pyrimidin-3-yl)phenyl)-3- (3-(trifluoromethyl)phenyl)urea (AD60); [0182] A synthetic strategy for Cmpd AD60 is depicted in Scheme 8 following. Scheme 8[0183] Reagent 3-iodo-lH-pyrazolo[3,4-d]pyrimidin-4-amine) (0.5g; 1.9 mmol; Apsel et al., 2008, Id.) was combined with cyclopentyl iodide (0.24 mL; 2.1 mmol), l .Og K2CO3, in 20 mL DMF and heated to 45 C under argon for 2 hours. The reaction was filtered to remove solid K2CO3, and the filtrate was combined with brine and the organic product was extracted in CH2Cl2 (3x 50 mL). The combined organic layer was concentrated in vacuo and purified by silica gel chromatography (MeOH/Chloroform; 5:95) to afford l-cyclopentyl-3- iodo-lH-pyrazolo[3,4-d]pyrimidin-4-amine (ESI-MS m/z [M+H]+ found 330.0, calculated 330.0). 4-nitrophenyl boronic acid (190 mg, 1.1 mmol; Sigma-Aldrich), was coupled to 1- cyclopentyl-3-iodo-lH-pyrazolo[3,4-d]pyrimidin-4-amine (150mg, 0.456 mmol) via the Suzuki reaction in 6 mL 1,2 methoxy ethane, 1 mL of saturated sodium carbonate, 1.65 mL EtOH, and 200 mg of polymer-bound tetrakis palladium. The reaction was stirred under argon for 12 hours at room temperature, filtered through Whatman paper to remove palladium, mixed with brine, extracted in chloroform and the product was subsequently purified on silica in EtOAc and concentrated in vacuo. The purified solid l~cyclopentyl-3-(4- nitrophenyl)-lH-pyrazolo[3,4-d]pyrimidin-4-amine (ESI-MS m/z [M+H]+ found 325.0, calculated 325.1 ; lOOmg, 0.31 mmol) was combined with Zinc dust (605 mg, 9.25 mmol), 10 mL THF, 0.35 mL HOAc for 12 hours at room temperature under Argon. The reaction was filtered through CeIi te, extracted with EtOAc and concentrated in vacuo to yield 3-(4- aminophenyl)-l -cyclopentyl- lH-pyrazolo [3, 4-d]pyrimidin-4-amine (ESI-MS m/z [M+H]+ found 295.0, calculated 295.2). To this reduced product, molar equivalents of3-(trifluoromethyl)phenyl isocyanate (Sigma-Aldrich) were added dropwise in ice-cold CH2C12. The reaction proceeded until completion as judged by TLC, was concentrated in vacuo, resuspended in 50:50 H20-CH3CN, and purified on a Cl 8 column in CH3CN/H20/0.1%TFA (1-100% gradient) to yield AD60 l-(4-(4-amino-l -cyclopentyl- IH- pyrazolo[3,4-d]pyrimidin-3-yl)phenyl)-3-(3-(trifluoromethyl)phenyl)urea (ESI-MS m/z [M+H]+ found 482.2, calculated 482.0).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,151266-23-8, its application will become more common.

Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; DAR, Arvin; SHOKAT, Kevan M.; WO2010/45542; (2010); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 151266-23-8, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 151266-23-8, name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine. A new synthetic method of this compound is introduced below.

Compound 2-4 is synthesized as shown in Scheme 2. Compound 1-3 is reacted with isopropyl bromide in dimethylformamide with potassium carbonate at 80 C., to provide the 1-isopropyl pyrazolopyrimidine intermediate, compound 2-1. This intermediate with the protected indolyl boronic acid species 2-2, using tetrakistriphenylphosphine palladium catalysis in DME-water solvent at 80 C. for 4-5 hours, to produce the Suzuki coupling product, compound 2-3. Removal of the protecting groups with acid in dioxane yields the product, 2-(4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl) iodide (Cpd. 2-4).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,151266-23-8, its application will become more common.

Reference:
Patent; The Regents of the University of California; Intellikine, Inc.; Shokat, Kevan M.; Fruman, David; Ren, Pingda; Wilson, Troy Edward; Li, Liansheng; Hsieh, Andrew; Feldman, Morris; Apsel, Beth; Liu, Yi; Rommel, Christian; Chan, Katrina; Ruggero, Davide; Pearce, David; Janes, Matthew; (84 pag.)US2016/789; (2016); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 151266-23-8, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 151266-23-8, Name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, SMILES is NC1=C2C(NN=C2I)=NC=N1, belongs to pyrimidines compound. In a article, author is Ghosh, Kalyan, introduce new discover of the category.

Chemical-informatics approach to COVID-19 drug discovery: Exploration of important fragments and data mining based prediction of some hits from natural origins as main protease (Mpro) inhibitors

As the world struggles against current global pandemic of novel coronavirus disease (COVID-19), it is challenging to trigger drug discovery efforts to search broad-spectrum antiviral agents. Thus, there is a need of strong and sustainable global collaborative works especially in terms of new and existing data analysis and sharing which will join the dots of knowledge gap. Our present chemical-informatics based data analysis approach is an attempt of application of previous activity data of SARS-CoV main protease (Mpro) inhibitors to accelerate the search of present SARS-CoV-2 Mpro inhibitors. The study design was composed of three major aspects: (1) classification QSAR based data mining of diverse SARS-CoV Mpro inhibitors, (2) identification of favourable and/or unfavourable molecular features/fingerprints/substructures regulating the Mpro inhibitory properties, (3) data mining based prediction to validate recently reported virtual hits from natural origin against SARS-CoV-2 Mpro enzyme. Our Structural and physico-chemical interpretation (SPCI) analysis suggested that heterocyclic nucleus like diazole, furan and pyridine have clear positive contribution while, thiophen, thiazole and pyrimidine may exhibit negative contribution to the SARS-CoV Mpro inhibition. Several Monte Carlo optimization based QSAR models were developed and the best model was used for screening of some natural product hits from recent publications. The resulted active molecules were analysed further from the aspects of fragment analysis. This approach set a stage for fragment exploration and QSAR based screening of active molecules against putative SARSCoV-2 Mpro enzyme. We believe the future in vitro and in vivo studies would provide more perspectives for anti-SARS-CoV-2 agents. (c) 2020 Elsevier B.V. All rights reserved.

Related Products of 151266-23-8, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 151266-23-8 is helpful to your research.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

151266-23-8, Name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C5H4IN5, SDS of cas: 151266-23-8, belongs to pyrimidines compound, is a common compound. In a patnet, author is de Sousa, Eduardo C., once mentioned the new application about 151266-23-8.

Nucleobase coupling by Mitsunobu reaction towards nucleoside analogs

The coupling of a nucleobase is a key step in the synthesis of most nucleoside analogs, e.g. carbocyclic nucleosides, isonucleosides and acyclic nucleosides. The synthetic strategies for nucleosides based on N-glycosylation are not applied when the nucleobase is not linked to the anomeric center. Thus, other methods have been employed, mainly those based on the alkylation of nucleobases. The Mitsunobu reaction, in which a hydroxy group is replaced by a nucleophile, has also been extensively applied, generating a diversity of molecules, including pharmaceuticals and their precursors. In this review the usefulness of this reaction for the coupling of nucleobases to non-anomeric positions of sugars, carbasugars and other homocyclic and linear structures is highlighted and discussed, covering purines and pyrimidines as pronucleophiles. [GRAPHICS] .

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 151266-23-8 help many people in the next few years. SDS of cas: 151266-23-8.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Chemistry is an experimental science, Recommanded Product: 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 151266-23-8, Name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C5H4IN5, belongs to pyrimidines compound. In a document, author is Xu, Chenhao.

Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing hydrazone fragment as potent and selective anticancer agents

In this paper, based on molecular hybridization, a series of [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing hydrazine was synthesized and their antiproliferative activities against 5 cancer cell lines (MGC-803, PC3, PC9, EC9706 and SMMC-7721) were evaluated. We found that most of them exhibited obvious growth inhibition effects on these tested cancer cells, especially compound 34 on PC3 cells (IC50 = 26.25 +/- 0.28 nM). Meanwhile, compound 34 displayed best selectivity on PC3, compared with the other cancer cell lines, as well as excellent selectivity towards normal cell lines (Het-1A, L02 and GES-1). Further investigations demonstrated that 34 could significantly inhibit PC3 cells’ colony formation, increase cellular ROS content, suppress EGFR expression and induce apoptosis. Our findings indicate that 34 may serve as a novel lead compound for the discovery of more triazolopyrimidine derivatives with improved anticancer potency and selectivity.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 151266-23-8, in my other articles. Recommanded Product: 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

151266-23-8, Name is 3-Iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C5H4IN5, Computed Properties of C5H4IN5, belongs to pyrimidines compound, is a common compound. In a patnet, author is Renthlei, Zothanmawii, once mentioned the new application about 151266-23-8.

Autophagy-deficient Arabidopsis mutant atg5, which shows ultraviolet-B sensitivity, cannot remove ultraviolet-B-induced fragmented mitochondria

Mitochondria damaged by ultraviolet-B radiation (UV-B, 280-315 nm) are removed by mitophagy, a selective autophagic process. Recently, we demonstrated that autophagy-deficient Arabidopsis thaliana mutants exhibit a UV-B-sensitive phenotype like that of cyclobutane pyrimidine dimer (CPD)-specific photolyase (PHR1)-deficient mutants. To explore the relationship between UV-B sensitivity and autophagy in UV-B-damaged plants, we monitored mitochondrial dynamics and autophagy in wild-type Arabidopsis (ecotype Columbia); an autophagy-deficient mutant, atg5; a PHR1-deficient mutant, phr1; an atg5 phr1 double mutant; and AtPHR1-overexpressing (AtPHR1ox) plants following high-dose UV-B exposure (1.5 W m(-2) for 1 h). At 10 h after exposure, the number of mitochondria per mesophyll leaf cell was increased and the volumes of individual mitochondria were decreased independently of UV-B-induced CPD accumulation in all genotypes. At 24 h after exposure, the mitochondrial number had recovered or almost recovered to pre-exposure levels in plants with functional autophagy (WT, phr1, and AtPHR1ox), but had increased even further in atg5. This suggested that the high dose of UV-B led to the inactivation and fragmentation of mitochondria, which were removed by mitophagy activated by UV-B. The UV-B-sensitive phenotype of the atg5 phr1 double mutant was more severe than that of atg5 or phr1. In wild-type, phr1, and AtPHR1ox plants, autophagy-related genes were strongly expressed following UV-B exposure independently of UV-B-induced CPD accumulation. Therefore, mitophagy might be one of the important repair mechanisms for UV-B-induced damage. The severe UV-B-sensitive phenotype of atg5 phr1 is likely an additive effect of deficiencies in independent machineries for UV-B protection, autophagy, and CPD photorepair.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 151266-23-8 help many people in the next few years. Computed Properties of C5H4IN5.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia