Category: 4045-24-3

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Sustainable Route Toward N-Boc Amines: AuCl3/CuI-Catalyzed N-tert-butyloxycarbonylation of Amines at Room Temperature, the main research direction is tertiary butoxycarbonyl amine preparation green chem; amine alc carbon monoxide tertiary butyloxycarbonylation gold copper catalyst; N-tert-butyloxycarbonylation; amines; gold catalysis; homogeneous catalysis; synergistic effect.Category: pyrrolines.

Herein, a step- and atom-economic synthesis of N-Boc amines RC(O)OC(CH3)3 (R = diethylaminyl, piperidin-1-yl, 4-methylpiperazin-1-yl, 1,4-dioxa-8-azaspiro[4.5]decan-8-yl, etc.) from amines RH, t-butanol, and CO was reported at room temperature Notably, this N-tert-butyloxycarbonylation procedure utilized ready-made substrates, com. available AuCl3/CuI as catalysts, and O2 from air as the sole oxidant. This catalytic system provided unique selectivity for N-Boc amines in good yields. More significantly, gram-scale preparation of medicinally important N-Boc amine intermediates was successfully implemented and, which demonstrated a potential application prospect in industrial syntheses. Furthermore, this approach also showed good compatibility with tertiary and other useful alcs. R1OH (R1 = t-Bu, 2-methylbutan-2-yl, Bn, etc.). Investigations of the mechanisms revealed that gold catalyzed the reaction and copper acted as electron transfer mediator in the catalytic cycle.

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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Discovery of a Novel and Brain-Penetrant O-GlcNAcase Inhibitor via Virtual Screening, Structure-Based Analysis, and Rational Lead Optimization, published in 2021-01-28, which mentions a compound: 4045-24-3, mainly applied to GlcNAcase inhibitor screening preparation tauopathy structure, Safety of 4-Methoxypiperidine.

O-GlcNAcase (OGA) has received increasing attention as an attractive therapeutic target for tau-mediated neurodegenerative disorders; however, its role in these pathologies remains unclear. Therefore, potent chem. tools with favorable pharmacokinetic profiles are desirable to characterize this enzyme. Herein, we report the discovery of a potent and novel OGA inhibitor, compound 5i, comprising an aminopyrimidine scaffold, identified by virtual screening based on multiple methodologies combining structure-based and ligand-based approaches, followed by sequential optimization with a focus on ligand lipophilicity efficiency. This compound was observed to increase the level of O-GlcNAcylated protein in cells and display suitable pharmacokinetic properties and brain permeability. Crystallog. anal. revealed that the chem. series bind to OGA via characteristic hydrophobic interactions, which resulted in a high affinity for OGA with moderate lipophilicity. Compound 5i could serve as a useful chem. probe to help establish a proof-of-concept of OGA inhibition as a therapeutic target for the treatment of tauopathies.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Organic Letters called Visible-Light-Induced Photoaddition of N-Nitrosoalkylamines to Alkenes: One-Pot Tandem Approach to 1,2-Diamination of Alkenes from Secondary Amines, Author is Patil, Dilip V.; Si, Tengda; Kim, Hun Young; Oh, Kyungsoo, which mentions a compound: 4045-24-3, SMILESS is COC1CCNCC1, Molecular C6H13NO, Electric Literature of C6H13NO.

The generation of aminium radical cation species from N-nitrosoamines is disclosed for the first time through visible-light excitation at 453 nm. The developed visible-light-promoted photoaddn. reaction of N-nitrosoamines to alkenes, e.g., 1H-Indene was combined with the o-NQ-catalyzed aerobic oxidation protocol of amines, e.g., 1,4-dioxa-8-azaspiro[4.5]decane to telescope the direct handling of harmful N-nitroso compounds, where the desired α-amino oxime derivatives e.g., I were obtained in a one-pot tandem N-nitrosation and photoaddn. sequence.

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Li, Xuemei; Hong, Duidui; Zhang, Mengmeng; Xu, Lei; Zhou, Yubo; Li, Jia; Liu, Tao published the article 《Development of peptide epoxyketones as selective immunoproteasome inhibitors》. Keywords: epoxyketone peptide synthesis peptidomimetic immunoproteasome inhibitor structure activity; antitumor agent drug design mol docking hydrogen bond chirality; isocyanate peptide coupling; Epoxyketones; Immunoproteasome inhibitor; Multiple myeloma; Selectivity.They researched the compound: 4-Methoxypiperidine( cas:4045-24-3 ).Product Details of 4045-24-3. 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:4045-24-3) here.

A series of epoxyketone analogs with varying N-caps and P3-configurations were designed, synthesized and evaluated. We found that D-Ala in P3 was crucial for β5i selectivity over β5c. Notably, compounds (I) (R1 = II) (β5i IC50 = 26.0 nM, 25-fold selectivity) and I (r1 = III) (β5i IC50 = 25.1 nM, 24-fold selectivity) with the D-configuration at P3 were the most selective inhibitors. Although I (R1 = II and III) showed only moderate anti-proliferative activity against RPMI-8226 and MM.1S cell lines, based on our experiments, it indicates that the inhibition of β5i alone is not sufficient to exert anticancer effects and may rely on the complementary inhibition of β1i, β5c and β5i. These data further increase our understanding of immunoproteasome inhibitors in hematol. malignancies.

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Application In Synthesis of 4-Methoxypiperidine. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities. Author is Wang, Pengxu; Batt, Sarah M.; Wang, Bin; Fu, Lei; Qin, Rongfei; Lu, Yu; Li, Gang; Besra, Gurdyal S.; Huang, Haihong.

In this study, we report the design and synthesis of a series of novel thiophene-arylamide compounds derived from the noncovalent decaprenylphosphoryl-β-D-ribose 2′-epimerase (DprE1) inhibitor TCA1 through a structure-based scaffold hopping strategy. Systematic optimization of the two side chains flanking the thiophene core led to new lead compounds bearing a thiophene-arylamide scaffold with potent antimycobacterial activity and low cytotoxicity. Compounds I, II, III [X = H,F] exhibited potent in vitro activity against both drug-susceptible (min. inhibitory concentration (MIC) = 0.02-0.12μg/mL) and drug-resistant (MIC = 0.031-0.24μg/mL) tuberculosis strains while retaining potent DprE1 inhibition (half maximal inhibitory concentration (IC50) = 0.2-0.9μg/mL) and good intracellular antimycobacterial activity. In addition, these compounds showed good hepatocyte stability and low inhibition of the human ether-á-go-go related gene (hERG) channel. The representative compound III [X = H] with acceptable pharmacokinetic property demonstrated significant bactericidal activity in an acute mouse model of tuberculosis. Moreover, the mol. docking study of template compound I provides new insight into the discovery of novel antitubercular agents targeting DprE1.

If you want to learn more about this compound(4-Methoxypiperidine)Application In Synthesis of 4-Methoxypiperidine, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(4045-24-3).

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SDS of cas: 4045-24-3. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer. Author is Yang, Huali; Wang, Xiaobing; Wang, Cheng; Yin, Fucheng; Qu, Lailiang; Shi, Cunjian; Zhao, Jinhua; Li, Shang; Ji, Limei; Peng, Wan; Luo, Heng; Cheng, Maosheng; Kong, Lingyi.

NUAK, the member of AMPK (AMP-activated protein kinase) family of protein kinases, is phosphorylated and activated by the LKB1 (liver kinase B1) tumor suppressor protein kinase. Recent work has indicated that NUAK1 is a key component of the antioxidant stress response pathway, and the inhibition of NUAK1 will suppress the growth and survival of colorectal tumors. As a promising target for anticancer drugs, few inhibitors of NUAK were developed. With this goal in mind, based on NUAK inhibitor WZ4003, a series of derivatives has been synthesized and evaluated for anticancer activity. Compound I, a derivative of WZ4003 by removing a methoxy group, was found to be the most potential one with stronger inhibitory against NUAK1/2 enzyme activity, tumor cell proliferation and inducing apoptosis of tumor cells. By in vivo efficacy evaluations of colorectal SW480 xenografts, I suppresses tumor growth more effectively with an excellent safety profile in vivo and is therefore seen as a suitable candidate for further investigation.

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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: 4045-24-3, is researched, Molecular C6H13NO, about Electrochemical Nonacidic N-Nitrosation/N-Nitration of Secondary Amines through a Biradical Coupling Reaction, the main research direction is nitroso amine green preparation crystal structure mol; amine biradical coupling electrochem nonacidic nitrosation; nitro azole green regioselective preparation crystal structure mol; azole biradical coupling electrochem nonacidic nitration.HPLC of Formula: 4045-24-3.

An acid-free N-nitrosation/nitration of the N-H bonds in secondary amines/azoles with Fe(NO3)3 · 9H2O as the nitroso/nitro source through an electrocatalyzed radical coupling reaction was developed to give nitroso-amines I [R = piperidin-1-yl, pyrrolidin-1-yl, morpholin-4-yl, etc.] and nitro-azoles II [R1 = 3-Me-pyrazol-1-yl, imidazol-1-yl, benzotriazol-1-yl, etc.] under mild conditions. Control and competition experiments, as well as kinetic studies demonstrated that N-nitrosation and N-nitration involved two different radical reaction pathways involving N+ and N. radicals. Moreover, the electrocatalysis method enabled the preferential activation of the N-H bond over the electrode and thus provided high selectivity for specific N atoms. This strategy exhibited a broad scope and provided a green and straightforward approach to generate useful compounds I and II in good yields.

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COA of Formula: C6H13NO. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Copper-Catalyzed 3-Positional Amination of 2-Azulenols with O-Benzoylhydroxylamines. Author is Li, Meng; Wang, Dong-Hui.

A copper-catalyzed ortho-selective amination of 2-azulenols with O-benzoylhydroxylamines (RR’N-OBz) to synthesize ortho-aminoazulenols was reported. A wide range of functional groups on amines were compatible, furnishing the corresponding amino-azulene derivatives in moderate to good yields. The further synthetic elaboration using 3-amino-2-azulenols as starting materials was demonstrated.

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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.Zhao, Ji-Ping; Ding, Lu-jia; Wang, Peng-Cheng; Liu, Ying; Huang, Min-Jun; Zhou, Xin-Li; Lu, Ming researched the compound: 4-Methoxypiperidine( cas:4045-24-3 ).Synthetic Route of C6H13NO.They published the article 《Electrochemical Nonacidic N-Nitrosation/N-Nitration of Secondary Amines through a Biradical Coupling Reaction》 about this compound( cas:4045-24-3 ) in Advanced Synthesis & Catalysis. Keywords: nitroso amine green preparation crystal structure mol; amine biradical coupling electrochem nonacidic nitrosation; nitro azole green regioselective preparation crystal structure mol; azole biradical coupling electrochem nonacidic nitration. We’ll tell you more about this compound (cas:4045-24-3).

An acid-free N-nitrosation/nitration of the N-H bonds in secondary amines/azoles with Fe(NO3)3 · 9H2O as the nitroso/nitro source through an electrocatalyzed radical coupling reaction was developed to give nitroso-amines I [R = piperidin-1-yl, pyrrolidin-1-yl, morpholin-4-yl, etc.] and nitro-azoles II [R1 = 3-Me-pyrazol-1-yl, imidazol-1-yl, benzotriazol-1-yl, etc.] under mild conditions. Control and competition experiments, as well as kinetic studies demonstrated that N-nitrosation and N-nitration involved two different radical reaction pathways involving N+ and N. radicals. Moreover, the electrocatalysis method enabled the preferential activation of the N-H bond over the electrode and thus provided high selectivity for specific N atoms. This strategy exhibited a broad scope and provided a green and straightforward approach to generate useful compounds I and II in good yields.

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Du, Lifei; Wang, Xiaoyu; Cui, Guonan; Xu, Bailing published an article about the compound: 4-Methoxypiperidine( cas:4045-24-3,SMILESS:COC1CCNCC1 ).Related Products of 4045-24-3. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:4045-24-3) through the article.

Pin1 is a peptidyl prolyl cis-trans isomerase (PPIase) and inhibiting Pin1 is a potential way for discovering anti-tumor agents. With an aim to find potent Pin1 inhibitors with a novel scaffold, a series of thiazole derivatives with an alicyclic heterocycles on the 2-position were designed, synthesized and tested against human Pin1. Compound 9p bearing a 2-oxa-6-azaspiro [3,3] heptane moiety on the thiazole scaffold was identified as the most potent Pin1 inhibitor of this series with an IC50 value of 0.95 μM. The structure-activity relationship (SAR) and mol. modeling study indicated that introducing an alicyclic ring with an H-bond acceptor would be a viable way to improve the binding affinity.

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