Category: 118430-74-3

Dang, Qun; Brown, Brian S.; Erion, Mark D. published the artcile< 5-Aminopyrazoles as Dienophiles in the Inverse Electron Demand Diels-Alder Reactions of 2,4,6-Tris(ethoxycarbonyl)-1,3,5-triazine: Syntheses of Pyrazolopyrimidines>, Computed Properties of 118430-74-3, the main research area is pyrazolopyrimidine preparation; cycloaddition ethoxycarbonyltriazine aminopyrazole; triazine trisethoxycarbonyl cycloaddition aminopyrazole; pyrazole amino cycloaddition trisethoxycarbonyltriazine.

[4 + 2] Cycloaddition reactions of 2,4,6-tris(ethoxycarbonyl)-1,3,5-triazine with 5-aminopyrazoles are reported. This methodol. is suitable for the one-step synthesis of highly substituted pyrazolo[3,4-d]pyrimidines.

Journal of Organic Chemistry published new progress about Diels-Alder reaction, inverse-electron-demand. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Computed Properties of 118430-74-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Fan, Wei; Ye, Qin; Xu, Hai-Wei; Jiang, Bo; Wang, Shu-Liang; Tu, Shu-Jiang published the artcile< Novel Double [3 + 2 + 1] Heteroannulation for Forming Unprecedented Dipyrazolo-Fused 2,6-Naphthyridines>, Quality Control of 118430-74-3, the main research area is double heterocyclization multicomponent domino reaction; dipyrazolo fused naphthyridine preparation.

A novel four-component strategy for the efficient synthesis of unprecedented dipyrazolo-fused 2,6-naphthyridines, e.g. I, through a double [3 + 2+1] heteroannulation has been described. The bond-forming efficiency, accessibility, and generality of this synthesis make it highly valuable to assemble tetra-heterocyclic scaffolds.

Organic Letters published new progress about Heterocyclization. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Quality Control of 118430-74-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Jiang, Bo; Fan, Wei; Sun, Mu-Yan; Ye, Qin; Wang, Shu-Liang; Tu, Shu-Jiang; Li, Guigen published the artcile< Domino Reaction of Arylglyoxals with Pyrazol-5-amines: Selective Access to Pyrazolo-Fused 1,7-Naphthyridines, 1,3-Diazocanes, and Pyrroles>, HPLC of Formula: 118430-74-3, the main research area is domino heterocyclization arylglyoxal pyrazolamine pyrazolo naphthyridine diazocane pyrrole.

New multicomponent domino reactions of arylglyoxals with pyrazol-5-amines have been established, providing selective access to unprecedented pyrazolo-fused 1,7-naphthyridines, 1,3-diazocanes, and pyrroles (up to 52 examples). The unreported dipyrazolo-fused 1,7-naphthyridines were regioselectively synthesized through a special double [3 + 2 + 1] heteroannulation accompanied by direct C-C formation between two electrophilic sites of arylglyoxals [e.g., PhCOCH(OH)2 + 1,3-dimethyl-5-pyrazolamine in presence of TsOH → I (70%)]. The unusual [3 + 3 + 1 + 1] cyclization resulted in 20 examples of novel dipyrazolo-fused 1,3-diazocanes [e.g., PhCOCH(OH)2 + 1-methyl-3-phenyl-5-pyrazolamine in presence of TsOH → II (71%)], whereas pyrrolo[2,3-c]pyrazoles were obtained in good yields by varying arylglyoxals and pyrazol-5-amines in the ratio 1:2 [e.g., PhCOCH(OH)2 + 1-phenyl-3-methyl-5-pyrazolamine in presence of TsOH → III (78%)]. Mechanisms of formation of these three new types of heterocycles are also proposed.

Journal of Organic Chemistry published new progress about Atom economy. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, HPLC of Formula: 118430-74-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Ding, Yun; Chai, Jing; Centrella, Paolo A.; Gondo, Chenaimwoyo; De Lorey, Jennifer L.; Clark, Matthew A. published the artcile< Development and Synthesis of DNA-Encoded Benzimidazole Library>, Computed Properties of 118430-74-3, the main research area is preparation DNA conjugated benzimidazole library NK3 receptor antagonist; DNA tagged fluoronitrobenzamide amine aldehyde; DNA-encoded library technology; benzimidazole.

Encoded library technol. (ELT) is an effective approach to the discovery of novel small-mol. ligands for biol. targets. A key factor for the success of the technol. is the chem. diversity of the libraries. Here we report the development of DNA-conjugated benzimidazoles. Using 4-fluoro-3-nitrobenzoic acid as a key synthon, we synthesized a 320 million-member DNA-encoded benzimidazole library using Fmoc-protected amino acids, amines and aldehydes as diversity elements. Affinity selection of the library led to the discovery of a novel, potent and specific antagonist of the NK3 receptor.

ACS Combinatorial Science published new progress about Chemical library. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Computed Properties of 118430-74-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Chen, Deheng; Lu, Tian; Yan, Ziqin; Lu, Wenchao; Zhou, Feilong; Lyu, Xilin; Xu, Biling; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng; Zhao, Yujun published the artcile< Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins>, SDS of cas: 118430-74-3, the main research area is benzodiazepine BET bromodomain BD2 protein inhibitor preparation cancer; BD2; BET protein; Bromodomain; Crystal structure; Selective.

Recently, selective inhibition of BET BD2 is emerging as a promising strategy for drug discovery. Despite significant progress in this area, systematic studies of selective BET BD2 inhibitors are still few. In this study, we report the discovery of a potent and selective BET BD2 inhibitor BY27 (47). Our high resolution co-crystal structures of 47/BRD2 BD1 and BD2 showed that the triazole group of 47, water mols., H433 and N429 in BRD2 BD2 established a water-bridged H-bonding network, which is responsible for the observed selectivities. DNA microarray anal. of HepG2 cells treated with 47 or OTX015 demonstrated the transcriptome impact differences between a BET BD2 selective inhibitor and a pan BET inhibitor. In a MV4-11 mouse xenograft model, 47 caused 67% of tumor growth inhibition and was less toxic than a pan BET inhibitor 1 at high doses. We conclude that the improved safety profile of selective BET BD2 inhibitors warrant future studies in BET associated diseases.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, SDS of cas: 118430-74-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Schulte, James P. II; Tweedie, Scott R. published the artcile< Palladium-catalyzed couplings of heteroaryl amines with aryl halides using sodium phenolate as the stoichiometric base>, Category: pyrazoles-derivatives, the main research area is microwave mediated palladium catalyzed coupling heteroaryl amine aryl halide; pyrazole pyridine pyrazine isoxazole arylamino preparation.

Heteroaryl amines are efficiently coupled (in two hours) to aryl halides with catalytic Pd2(dba)3 and Xantphos to provide the corresponding biaryl amines under microwave and standard thermal conditions. E.g., 3-tert-butyl-1-methyl-1H-pyrazol-5-amine reacts with p-bromobenzonitrile in the presence of 1.25 mol% Pd2(dba)3, 3 mo% Xantphos ligand and 1,5 equivalent NaOPh/dioxane under microwave conditions to give 91% yield of biarylamine I. The use of organic-soluble Na phenolate (NaOPh) as the stoichiometric base promotes facile coupling of a variety of substrates in excellent yields.

Synlett published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent) (heteroaryl). 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Category: pyrazoles-derivatives.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Jiang, Bo; Ye, Qin; Fan, Wei; Wang, Shu-Liang; Tu, Shu-Jiang; Li, Guigen published the artcile< Four-component strategy for selective synthesis of azepino[5,4,3-cd]indoles and pyrazolo[3,4-b]pyridines>, Electric Literature of 118430-74-3, the main research area is pyrazolamine arylglyoxal hydrate aniline multicomponent domino cyclocondensation; hydropyrazoloazepinoindole preparation; pyrazolopyridine preparation.

A novel four-component strategy for the selective synthesis of fused 1,5,9,10-tetrahydropyrazolo[4′,3′:6,7]azepino[5,4,3-cd]indoles and pyrazolo[3,4-b]pyridines by domino reactions of 1-substituted 5-pyrazolamines, arylglyoxal monohydrates, and anilines was established. The bond-forming efficiency, accessibility of starting materials and substrate scope provide invaluable access to tetra-, and bis-heterocyclic scaffolds.

Chemical Communications (Cambridge, United Kingdom) published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Electric Literature of 118430-74-3.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 118430-74-3, name is 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine belongs to pyrazoles-derivatives compound, it is a common compound, a new synthetic route is introduced below. HPLC of Formula: C7H11N3

Example 161 Synthesis of N4-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-9H-pyrimido[4,5-b]indole-2,4-diamine (Cpd. No. 206) Pd2(dba)3 (18 mg) and BINAP (26 mg) were mixed in anhydrous toluene. And the mixture was heated at reflux for 3-4 minutes. This mixture was transferred into a round-bottom flask containing ZBB253 (60 mg), 3-cyclopropyl-1-methyl-1H-pyrazol-5-amine (84 mg), K3PO4 (130 mg), and toluene (2 mL). The mixture was heated at reflux for overnight before quenching with methanol. The reaction mixture was filtered and the mixture was purified by HPLC to yield Cpd. No. 206 as a CF3CO2H salt in 15 mg. ESI-MS calculated for C23H25N8O2 [M+H]+=445.21; Observed: 445.54. 1H NMR (300 MHz, MeOD) delta 7.70 (s, 1H), 7.35 (s, 1H), 6.09 (s, 1H), 3.92 (s, 3H), 3.74 (s, 3H), 2.33 (s, 3H), 2.16 (s, 3H), 1.98-1.88 (m, 1H), 1.03-0.93 (m, 2H), 0.78-0.71 (m, 2H).

The synthetic route of 118430-74-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF MICHIGAN; Wang, Shaomeng; Zhao, Yujun; Zhou, Bing; Aguilar, Angelo; Liu, Liu; Bai, Longchuan; McEachern, Donna; Sun, Duxin; Wen, Bo; Luo, Ruijuan; Zhao, Ting; Chinnaiyan, Arul; Asangani, Irfan A.; Stuckey, Jeanne; Meagher, Jennifer Lynn; Ran, Xu; US2015/246923; (2015); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 118430-74-3, name is 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, belongs to pyrazoles-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 118430-74-3, SDS of cas: 118430-74-3

Synthesis of N-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-2-((methylsulfonyl)methyl)-9H-pyrimido[4,5-b]indol-4-amine (Cpd. No. 289) Pd2(dba)3 (18 mg) and BINAP (26 mg) were mixed in anhydrous toluene. And the mixture was heated at reflux for 3-4 minutes. This mixture was transferred into a round-bottom flask containing ZBB273 (60 mg), 3-cyclopropyl-1-methyl-1H-pyrazol-5-amine (84 mg), K3PO4 (130 mg), and toluene (4 mL). The mixture was heated at reflux for overnight before quenching with methanol. The reaction mixture was filtered and the mixture was purified by HPLC to yield Cpd. No. 289 as a CF3CO2H salt in 27 mg. ESI-MS calculated for C25H28N7O4S [M+H]+=522.19; Observed: 522.44.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, and friends who are interested can also refer to it.

Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF MICHIGAN; Wang, Shaomeng; Zhao, Yujun; Zhou, Bing; Aguilar, Angelo; Liu, Liu; Bai, Longchuan; McEachern, Donna; Sun, Duxin; Wen, Bo; Luo, Ruijuan; Zhao, Ting; Chinnaiyan, Arul; Asangani, Irfan A.; Stuckey, Jeanne; Meagher, Jennifer Lynn; Ran, Xu; US2015/246923; (2015); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 118430-74-3, name is 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, belongs to pyrazoles-derivatives compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 118430-74-3, name: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine

Synthesis of N-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethylisoxazol-4-yl)-6-methoxy-2-((methylsulfonyl)methyl)-9H-pyrimido[4,5-b]indol-4-amine (Cpd. No. 289) Pd2(dba)3 (18 mg) and BINAP (26 mg) were mixed in anhydrous toluene. And the mixture was heated at reflux for 3-4 minutes. This mixture was transferred into a round-bottom flask containing ZBB273 (60 mg), 3-cyclopropyl-1-methyl-1H-pyrazol-5-amine (84 mg), K3PO4 (130 mg), and toluene (4 mL). The mixture was heated at reflux for overnight before quenching with methanol. The reaction mixture was filtered and the mixture was purified by HPLC to yield Cpd. No. 289 as a CF3CO2H salt in 27 mg. ESI-MS calculated for C25H28N7O4S [M+H]+=522.19; Observed: 522.44.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, and friends who are interested can also refer to it.

Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF MICHIGAN; Wang, Shaomeng; Zhao, Yujun; Zhou, Bing; Aguilar, Angelo; Liu, Liu; Bai, Longchuan; McEachern, Donna; Sun, Duxin; Wen, Bo; Luo, Ruijuan; Zhao, Ting; Chinnaiyan, Arul; Asangani, Irfan A.; Stuckey, Jeanne; Meagher, Jennifer Lynn; Ran, Xu; US2015/246923; (2015); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics