Category: 4045-24-3

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Methoxypiperidine(SMILESS: COC1CCNCC1,cas:4045-24-3) is researched.Recommanded Product: 58081-05-3. The article 《Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:4045-24-3).

As abnormal PI3K signaling is a feature of many types of cancer, the development of orally active PI3K inhibitors is of great significance for targeted cancer therapy. Through integrating strategies of reducing aromatic character/increasing the fraction of sp3 carbons together with scaffold hopping, we designed and synthesized two new series of thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives for use as PI3K inhibitors. Our structure-activity relationship studies led to the identification of thieno[2,3-d]pyrimidine 6a and thiazolo[5,4-d]pyrimidine 7a (I and II, resp.), which exhibited remarkable nanomolar PI3K potency, good antiproliferative activity, favorable pharmacokinetic properties and significant in vivo anti-cancer efficacy. Notably, thiazolo[5,4-d]pyrimidine 7a had better anti-cancer activity than thieno[2,3-d]pyrimidine 6a and is worthy of further pre-clin. evaluation for its use in cancer treatment.

The article 《Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors》 also mentions many details about this compound(4045-24-3)Formula: C6H13NO, you can pay attention to it or contacet with the author([email protected]; [email protected]; [email protected]) to get more information.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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 Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer, the main research direction is pyrimidine human colorectal cancer anticancer apoptosis; AMP-Activated protein kinase (AMPK); Colorectal cancer; NUAK; WZ4003 derivatives.Application of 4045-24-3.

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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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 4-Methoxypiperidine(SMILESS: COC1CCNCC1,cas:4045-24-3) is researched.Application of 4045-24-3. The article 《Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis》 in relation to this compound, is published in European Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:4045-24-3).

A series of thiophene-benzenesulfonamide derivatives was designed and synthesized by exploring the structure-activity relationship of lead compounds 2,3-disubstituted thiophenes I and 297F II as antituberculosis agents, which displayed potent antimycobacterial activity against drug-susceptible and clin. isolated drug-resistant tuberculosis. In particular, compound III (-R1R2- = -(CH2)4-), which had improved activity (min. inhibitory concentration of 0.023 μg/mL) compared with the lead compounds, displayed good intracellular antimycobacterial activity in macrophages with a reduction of 1.29 log10 CFU. A druggability evaluation indicated that compound III (-R1R2- = -(CH2)4-) had favorable hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. Moreover, compound III (-R1R2- = -(CH2)4-) exhibited modest in vivo efficacy in an acute mouse model of tuberculosis. In addition, the mol. docking study elucidated the binding mode of compound III (-R1R2- = -(CH2)4-) in the active site of DprE1. Therefore, compound III (-R1R2- = -(CH2)4-) may be a promising antituberculosis lead for further research.

The article 《Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis》 also mentions many details about this compound(4045-24-3)Recommanded Product: 4-Methoxypiperidine, you can pay attention to it or contacet with the author([email protected]; [email protected]; [email protected]) to get more information.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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 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, Name is 4-Methoxypiperidine, Molecular C6H13NO, Recommanded Product: 4045-24-3.

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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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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: 4045-24-3, is researched, SMILESS is COC1CCNCC1, Molecular C6H13NOJournal, Advanced Synthesis & Catalysis called Electrochemical Nonacidic N-Nitrosation/N-Nitration of Secondary Amines through a Biradical Coupling Reaction, Author is Zhao, Ji-Ping; Ding, Lu-jia; Wang, Peng-Cheng; Liu, Ying; Huang, Min-Jun; Zhou, Xin-Li; Lu, Ming, 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.Recommanded Product: 4-Methoxypiperidine.

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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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Lanthanide-Catalyzed Tandem Addition of Amines to Cyanoalkenes: Synthesis of Cyclic Amidines》. Authors are Hou, Jinsong; Yang, Gaosheng; Chai, Zhuo.The article about the compound:4-Methoxypiperidinecas:4045-24-3,SMILESS:COC1CCNCC1).Related Products of 4045-24-3. Through the article, more information about this compound (cas:4045-24-3) is conveyed.

A tandem insertion of aliphatic nitriles and unactivated alkenes RCH(CN)CH2C(R1)=C(R2)R3 (R = Ph, 2-thienyl, 3-pyridinyl, etc.; R1 = H, Me; R2 = H, Me, Ph, 2-naphthyl, etc.; R3 = H, Me) to the N-H bond of secondary aliphatic amines such as dibenzylamine, pyrrolidine, thiomorpholine, etc. catalyzed by simple trialkyl rare-earth metal complexes was disclosed. This reaction provides a highly atom-economic and stereoselective way to a range of cyclic amidines I (R4 = benzyl(methyl)aminyl, tetrahydroisoquinolin-2-yl, thiomorpholin-4-yl, etc.) under mild reaction conditions.

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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

Electric Literature of C6H13NO. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Palladium-Catalyzed C-H Amination/[2+3] or [2+4] Cyclization via C(sp3 or sp2)-H Activation. Author is An, Yang; Li, Yuke; Zhang, Xiao-Yan; Zhang, Zhe; Gou, Xue-Ya; Ding, Ya-Nan; Li, Qiao; Liang, Yong-Min.

This report describes a palladium-catalyzed Catellani reaction consisting of amination/[2+3] or [2+4] cyclization via a carboxylate ligand-exchange strategy. This method effectively activates ortho-substituents that avoid a second C-H palladation. The scope of substrates was broad, o-methyl-substituted iodoarenes R-2-CH3-C6H3I (R = H, 4-F, 3-Me, 4-Cl, etc.), 3-iodo-4-methyl-pyridine were applied to the reaction smoothly, and o-phenyl-substituted iodoarenes 2-I-C6H4-(4-R1C6H4-) (R1 = H, Me, Ph, F, etc.), 1-(2-iodo-phenyl)-naphthalene can also be obtained by this method. In terms of mechanism, d. functional theory calculations proved the sequence of the key five-membered aryl-norbornene-palladacycle intermediate formation and C(sp3 or sp2)-H activation.

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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

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 Copper-Catalyzed Aminoarylation of Alkenes via Aminyl Radical Addition and Aryl Migration, the main research direction is amino amide preparation; alkene hydroxylamine copper catalyst aminoarylation.Name: 4-Methoxypiperidine.

A new strategy for aminoarylation of alkenes by copper-catalyzed SMILESs rearrangement using O-benzoylhydroxylamines as the amine reagent was described.. This method affords various β-amino amide derivatives possessing a quaternary carbon center with wide functional group tolerance and high regioselectivity. The mechanistic studies indicate that the transformation can involve aminyl radical intermediates under acid-free condition.

After consulting a lot of data, we found that this compound(4045-24-3)Name: 4-Methoxypiperidine can be used in many types of reactions. And in most cases, this compound has more advantages.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

Recommanded Product: 4045-24-3. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Development of peptide epoxyketones as selective immunoproteasome inhibitors. Author is Li, Xuemei; Hong, Duidui; Zhang, Mengmeng; Xu, Lei; Zhou, Yubo; Li, Jia; Liu, Tao.

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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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem

Name: 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 Copper-Catalyzed ortho-Selective Dearomative C-N Coupling of Simple Phenols with O-Benzoylhydroxylamines. Author is Yao, Zhi-Li; Wang, Lei; Shao, Nan-Qi; Guo, Yin-Long; Wang, Dong-Hui.

In the presence of Cu(OTf)2 and LiOt-Bu in THF, 2,6-disubstituted phenols such as 2,6-dimethylphenol underwent regioselective dearomative coupling reactions with secondary O-benzoylhydroxylamines such as 4-(benzoyloxy)morpholine to yield aminocyclohexadienones such as I. Lack of inhibition with radical trapping agents, lack of rearrangement with a cyclopropylated phenol, and mass spectrometric detection of intermediates in the reaction support a mechanism involving either a single-electron transfer process involving attack of an N-centered radical onto the phenol or a two-electron pathway involving addition of phenol to an electrophilic Cu(III)-amino complex via an inner-sphere process.

Although many compounds look similar to this compound(4045-24-3)Name: 4-Methoxypiperidine, numerous studies have shown that this compound(SMILES:COC1CCNCC1), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem