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Application of 159326-69-9. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Copper(II)-catalyzed cascade approach for the synthesis of pyrrolo[2,1-f][1,2,4]triazine-fused isoquinolines.

A copper(II)-catalyzed coupling-cyclization reaction that allowed a facile access to an impressive variety of pyrrolo[2,1-f][1,2,4]triazine-fused isoquinolines, e.g., I, in good to excellent yields has been developed. The reaction proceeded with high 6-endo-dig regioselectivity, and the product was confirmed by x-ray crystallog. study. This method appeared to be compatible with different substituted starting materials that have different electronic properties, increasing its applicability to various functional groups.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Holmes, Jane L.; Almeida, Lynsie; Barlaam, Bernard; Croft, Rosemary A.; Dishington, Allan P.; Gingipalli, Laksmaiah; Hassall, Lorraine A.; Hawkins, Janet L.; Ioannidis, Stephanos; Johannes, Jeffrey W.; McGuire, Thomas M.; Moore, Jane E.; Patel, Anil; Pike, Kurt G.; Pontz, Timothy; Wu, Xiaoyun; Wang, Tao; Zhang, Hai-Jun; Zheng, Xiaolan researched the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ).Electric Literature of C5H7N3O.They published the article 《Synthesis of Novel Hydroxymethyl-Substituted Fused Heterocycles》 about this compound( cas:159326-69-9 ) in Synthesis. Keywords: fused heterocycle preparation. We’ll tell you more about this compound (cas:159326-69-9).

Examples of hydroxymethylated analogs of heteroaryl cores such as quinazolin-4-ones, isoquinolin-1(2H)-ones, pyrido[3,4-d]pyrimidin-4(3H)-ones, chromen-4-ones and pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones were sparse or non-existent in the scientific literature. Synthesis of such compounds by using standard procedures from readily available raw materials was demonstrated.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ) is researched.Category: thiazole.Chen, Yanhong; Xiang, Haoyue; Tan, Cun; Xie, Yuyuan; Yang, Chunhao published the article 《A tandem copper (II)-promoted synthesis of 2-substituted pyrrolo[2,1-f][1,2,4] triazin-4(3H)-ones》 about this compound( cas:159326-69-9 ) in Tetrahedron. Keywords: aldehyde aminopyrroleamide annulation cupric chloride catalyst; acetal aminopyrroleamide annulation cupric chloride catalyst; pyrrolotriazinone preparation. Let’s learn more about this compound (cas:159326-69-9).

Annulation of 1-amino-1H-pyrrole-2-amides with various substituted benzaldehydes, heteroaryl aldehydes, alkyl aldehydes or even acetals, promoted by cupric chloride, to synthesize 2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones was carried out. This approach provides a useful method for constructing the privileged structure in medicinal chem. Electron-donating groups on both partners could accelerate the reaction.

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Jia, Hong; Dai, Guangxiu; Su, Weiguo; Xiao, Kun; Weng, Jianyang; Zhang, Zhulin; Wang, Qing; Yuan, Tianhai; Shi, Fuying; Zhang, Zheng; Chen, Wei; Sai, Yang; Wang, Jian; Li, Xiong; Cai, Yu; Yu, Jun; Ren, Ping; Venable, Jennifer; Rao, Tadimeti; Edwards, James P.; Bembenek, Scott D. published the article 《Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors》. Keywords: pyrrolotriazinone synthesis SAR pharmacokinetics PI3K rheumatoid arthritis autoimmune disorders.They researched the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ).Product Details of 159326-69-9. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:159326-69-9) here.

An electronic d. model was developed and used to identify a novel pyrrolotriazinone replacement for a quinazolinone, a commonly used moiety to impart selectivity in inhibitors for PI3Kγ and PI3Kδ. Guided by mol. docking, this new specificity piece was then linked to the hinge-binding region of the inhibitor using a novel cyclic moiety. Further structure-activity relationship optimization around the hinge region led to the discovery of candidate 26, a highly potent and selective PI3Kγ-PI3Kδ dual inhibitor with favorable drug metabolism and pharmacokinetic properties in preclin. species.

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Annulation of 1-amino-1H-pyrrole-2-amides with various substituted benzaldehydes, heteroaryl aldehydes, alkyl aldehydes or even acetals, promoted by cupric chloride, to synthesize 2-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones was carried out. This approach provides a useful method for constructing the privileged structure in medicinal chem. Electron-donating groups on both partners could accelerate the reaction.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 159326-69-9, is researched, Molecular C5H7N3O, about Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template, the main research direction is pyrrolotriazine derivative preparation structure activity VEGF EGFR kinase antitumor.Quality Control of 1-Aminopyrrole-2-carboxamide.

The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline kinase inhibitor scaffold. Attachment of a 4-((3-chloro-4-fluorophenyl)amino) substituent to the template provided potent biochem. inhibitors of the tyrosine kinase activity of EGFR, as well as inhibition of cellular proliferation of the human colon tumor cell line DiFi. Attachment of a 4-((3-hydroxy-4-methylphenyl)amino) substituent provided potent inhibitors of VEGFR-2 which also showed effects on the VEGF-dependent proliferation of human umbilical vein endothelial cells. Biol. activity was maintained with substitution at positions 5 or 6, but not 7, suggesting that the former positions are promising sites for introducing side chains which modulate physicochem. properties. Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.

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A diversity-oriented approach to the synthesis of pyrimidinyl-/pyrazolyl-substituted pyrrolo[2,1-f][1,2,4]triazin-4(3H)-ones, e.g., I and II, via copper-promoted two-step one-pot reaction of chromones with pyrrolecarboxamides and amidines/hydrazines was developed. Pot, atom and step economy were combined in these sequential reactions, and at least six bonds were formed in one pot.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 159326-69-9, is researched, SMILESS is O=C(C1=CC=CN1N)N, Molecular C5H7N3OJournal, RSC Advances called Copper(II)-catalyzed cascade approach for the synthesis of pyrrolo[2,1-f][1,2,4]triazine-fused isoquinolines, Author is Chen, Jianyang; Liu, Bo; Chen, Yanhong; He, Qian; Yang, Chunhao, the main research direction is pyrrolo triazine fused isoquinoline one pot tandem regioselective preparation; alkynylbenzaldehyde amino pyrrolecarboxamide condensation nucleophilic addition cyclization copper catalyst.Application In Synthesis of 1-Aminopyrrole-2-carboxamide.

A copper(II)-catalyzed coupling-cyclization reaction that allowed a facile access to an impressive variety of pyrrolo[2,1-f][1,2,4]triazine-fused isoquinolines, e.g., I, in good to excellent yields has been developed. The reaction proceeded with high 6-endo-dig regioselectivity, and the product was confirmed by x-ray crystallog. study. This method appeared to be compatible with different substituted starting materials that have different electronic properties, increasing its applicability to various functional groups.

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Hunt, John T.; Mitt, Toomas; Borzilleri, Robert; Gullo-Brown, Johnni; Fargnoli, Joseph; Fink, Brian; Han, Wen-Ching; Mortillo, Steven; Vite, Gregory; Wautlet, Barri; Wong, Tai; Yu, Chiang; Zheng, Xiaoping; Bhide, Rajeev published the article 《Discovery of the Pyrrolo[2,1-f][1,2,4]triazine Nucleus as a New Kinase Inhibitor Template》. Keywords: pyrrolotriazine derivative preparation structure activity VEGF EGFR kinase antitumor.They researched the compound: 1-Aminopyrrole-2-carboxamide( cas:159326-69-9 ).Reference of 1-Aminopyrrole-2-carboxamide. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:159326-69-9) here.

The pyrrolo[2,1-f][1,2,4]triazine nucleus was identified as a novel kinase inhibitor template which effectively mimics the well-known quinazoline kinase inhibitor scaffold. Attachment of a 4-((3-chloro-4-fluorophenyl)amino) substituent to the template provided potent biochem. inhibitors of the tyrosine kinase activity of EGFR, as well as inhibition of cellular proliferation of the human colon tumor cell line DiFi. Attachment of a 4-((3-hydroxy-4-methylphenyl)amino) substituent provided potent inhibitors of VEGFR-2 which also showed effects on the VEGF-dependent proliferation of human umbilical vein endothelial cells. Biol. activity was maintained with substitution at positions 5 or 6, but not 7, suggesting that the former positions are promising sites for introducing side chains which modulate physicochem. properties. Preliminary inhibition studies with varying ATP concentrations suggest that, like the quinazoline-based kinase inhibitors, the pyrrolotriazine-based inhibitors bind in the ATP pocket.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 1-Aminopyrrole-2-carboxamide, is researched, Molecular C5H7N3O, CAS is 159326-69-9, about Design, synthesis, and evaluation of pyrrolo[2,1-f][1,2,4]triazine derivatives as novel hedgehog signaling pathway inhibitors, the main research direction is pyrrolotriazine derivative preparation SAR hedgehog signaling inhibitor cancer; Hedgehog signaling pathway; Inhibitors; Novel; Pyrrolo[2,1-f][1,2,4]triazine.Recommanded Product: 159326-69-9.

A novel series of Hh signaling pathway inhibitors were designed by replacing the pyrimidine skeleton of our earlier reported lead compound with pyrrolo[2,1-f][1,2,4]triazine scaffold. Starting from this new scaffold, SAR exploration was investigated based on structural modification on A-ring, C-ring and D-ring. And several much potent compounds were studies in vivo to profile their pharmacokinetic properties. Finally, optimization leads to the identification of compound (I), a potent Hh signaling pathway inhibitor with superior potency in vitro and satisfactory pharmacokinetic properties in vivo.

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