Category: 118994-89-1

Edney, Dean; Hulcoop, David G.; Leahy, John H.; Vernon, Lois E.; Wipperman, Mark D.; Bream, Robert N.; Webb, Michael R. published the article 《Development of Flexible and Scalable Routes to Two Phosphatidinylinositol-3-kinase Delta Inhibitors via a Common Intermediate Approach》. Keywords: oxazolylindazole preparation; pyridinylborate haloindazoyloxazole Suzuki coupling.They researched the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ).Recommanded Product: 118994-89-1. 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:118994-89-1) here.

This paper describes the discovery and development of a flexible route to two candidate drug mols. by a common intermediate approach. Key reactions include Negishi and Suzuki couplings to form biaryl bonds. Conditions for a Miyaura borylation of heteroaryl bromides were also developed. Heteroaryl trifluoroborates and aryl chlorides were used as coupling partners in the Suzuki reaction, thereby minimizing detrimental side reactions such as protodeboronation and oxidative homocoupling. A complementary set of reaction conditions using pinacolboronates with potassium bifluoride as an additive were also developed and used to make 5 kg of drug substance for use in early-phase clin. trials.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Direct amidation of azoles with formamides via metal-free C-H activation in the presence of tert-butyl perbenzoate, the main research direction is direct amidation azole formamide reactant azolecarboxamide preparation; tertbutyl perbenzoate oxidant amidation azole formamide reactant; cross coupling azolecarboxamide preparation tertbutyl perbenzoate oxidant.SDS of cas: 118994-89-1.

A novel and simple method for the direct amidation of azoles with formamides has been developed. The reaction could occur smoothly in the presence of tert-Bu perbenzoate (TBPB) as an oxidant under metal- and base-free conditions. Direct dehydrogenative cross-coupling of formamides and azoles generated the corresponding products, e.g. I (X = S, R = Me2N, EtNH; X = O, R = 2-MeC6H4NH, Et2N), in good yields.

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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: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ) is researched.Name: Ethyl oxazole-5-carboxylate.Li, Chengliang; Li, Pinhua; Yang, Jin; Wang, Lei published the article 《Palladium-catalyzed deamidative arylation of azoles with arylamides through a tandem decarbonylation-C-H functionalization》 about this compound( cas:118994-89-1 ) in Chemical Communications (Cambridge, United Kingdom). Keywords: azole arylamide palladium chemoselective regioselective deamidative arylation; aryl azole preparation; chemoselective regioselective deamidative arylation catalyst palladium. Let’s learn more about this compound (cas:118994-89-1).

A highly chemo-, regio-selective, and efficient palladium-catalyzed deamidative arylation of azoles with arylamides, as an aryl metal equivalent, has been developed. The reaction proceeds smoothly to generate the corresponding products in good yields via a tandem decarbonylation-C-H activation.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis, published in 2021-03-19, which mentions a compound: 118994-89-1, Name is Ethyl oxazole-5-carboxylate, Molecular C6H7NO3, COA of Formula: C6H7NO3.

A practical approach toward the synthesis of 2-arylazoles via direct arylation was described. The transformation relied on a Pd/Cu cocatalyst system that operated with low catalyst loadings. The reaction conditions were found to be tolerant of a wide range of functional groups and nitrogen-containing heterocycles commonly employed in a drug discovery setting.

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Synthesis and evaluation of anthelmintic and cytotoxic properties of [2,5′]bis-1,3-azole analogs of bengazoles.Synthetic Route of C6H7NO3.

Using different heterocycle formation methodologies (Deoxo-Fluor, DAST, POCl3, TosMIC), [2,5′]bis-1,3-azoles were prepared as stable analogs of bengazoles, a family of potent anthelmintic marine natural products. The cytotoxic activity of these heterocycles and their precursors on HCT-15 cells and the effect on the L4 larvae of Nippostrongylus brasiliensis were evaluated.

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Recommanded Product: 118994-89-1. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Palladium-catalyzed intermolecular carbonylative cross-coupling of heteroaryl C(sp2)-H bonds with amines: an efficient strategy for oxidative aminocarbonylation of azoles. Author is Xing, Qi; Lv, Hui; Xia, Chungu; Li, Fuwei.

An efficient palladium-catalyzed oxidative aminocarbonylation of azoles such as benzothiazole, 5-chloro benzoxazole, 4,5-dimethyl-1,3-thiazole, etc. has been developed. This system allows for intermol. carbonylative cross-coupling of aromatic C(sp2)-H bonds with simple amines RR1NH [R = H, CH2CH3, c-C6H11, etc.; R1 = C(H3)3, (CH2)2CH3, CH2C6H5, etc.; RR1 = -(CH2)2O(CH2)2-, -(CH2)5-], which has often been asked for, but has not been realized so far. It provides a straightforward approach to a variety of azol-2-amides RR1NC(O)R2 (R2 = 1,3-benzothiazol-2-yl, 5-chloro-1,3-benzoxazol-2-yl, dimethyl-1,3-thiazol-2-yl, etc.).

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Application In Synthesis of Ethyl oxazole-5-carboxylate. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Nickel-catalyzed decarboxylative acylation of heteroarenes by sp2 C-H functionalization. Author is Yang, Ke; Zhang, Cheng; Wang, Peng; Zhang, Yan; Ge, Haibo.

Nickel-catalyzed ligand-free decarboxylative cross-coupling of azole derivatives with α-oxoglyoxylic acids was developed. This work represents the first example of decarboxylative cross-coupling reactions, in a C-H bond functionalization manner, through nickel catalysis, and tolerates various functional groups. Addnl., this approach provides an efficient access to (ox)azole ketones, an important structural motif in many medicinal compounds with a broad range of biol. activities. © 2014 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

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Pyrazine – Wikipedia,
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Recommanded Product: 118994-89-1. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Discovery of Novel 1,4-Diacylpiperazines as Selective and Cell-Active eIF4A3 Inhibitors. Author is Ito, Masahiro; Tanaka, Toshio; Cary, Douglas R.; Iwatani-Yoshihara, Misa; Kamada, Yusuke; Kawamoto, Tomohiro; Aparicio, Samuel; Nakanishi, Atsushi; Imaeda, Yasuhiro.

Eukaryotic initiation factor 4A3 (eIF4A3), a member of the DEAD-box RNA helicase family, is one of the core components of the exon junction complex (EJC). The EJC is known to be involved in a variety of RNA metabolic processes typified by nonsense-mediated RNA decay (NMD). In order to identify mol. probes to investigate the functions and therapeutic relevance of eIF4A3, a search for selective eIF4A3 inhibitors was conducted. Through the chem. optimization of 1,4-diacylpiperazine derivatives identified via high-throughput screening (HTS), we discovered the first reported selective eIF4A3 inhibitor 53a exhibiting cellular NMD inhibitory activity. A surface plasmon resonance (SPR) biosensing assay ascertained the direct binding of 53a and its analog 52a to eIF4A3 and revealed that the binding occurs at a non-ATP binding site. Compounds 52a and 53a represent novel mol. probes for further study of eIF4A3, the EJC, and NMD.

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Pyrazine – Wikipedia,
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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Palladium-catalyzed deamidative arylation of azoles with arylamides through a tandem decarbonylation-C-H functionalization, the main research direction is azole arylamide palladium chemoselective regioselective deamidative arylation; aryl azole preparation; chemoselective regioselective deamidative arylation catalyst palladium.Safety of Ethyl oxazole-5-carboxylate.

A highly chemo-, regio-selective, and efficient palladium-catalyzed deamidative arylation of azoles with arylamides, as an aryl metal equivalent, has been developed. The reaction proceeds smoothly to generate the corresponding products in good yields via a tandem decarbonylation-C-H activation.

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Pyrazine – Wikipedia,
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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.Piou, Tiffany; Slutskyy, Yuriy; Kevin, Nancy J.; Sun, Zhongxiang; Xiao, Dong; Kong, Jongrock researched the compound: Ethyl oxazole-5-carboxylate( cas:118994-89-1 ).Application of 118994-89-1.They published the article 《Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis》 about this compound( cas:118994-89-1 ) in Organic Letters. Keywords: oxazole aryl halide palldium copper catalyst arylation; ethyl aryl oxazole carboxylate preparation. We’ll tell you more about this compound (cas:118994-89-1).

A practical approach toward the synthesis of 2-arylazoles via direct arylation was described. The transformation relied on a Pd/Cu cocatalyst system that operated with low catalyst loadings. The reaction conditions were found to be tolerant of a wide range of functional groups and nitrogen-containing heterocycles commonly employed in a drug discovery setting.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem