Category: 4045-24-3

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Methoxypiperidine( cas:4045-24-3 ) is researched.Name: 4-Methoxypiperidine.An, Yang; Li, Yuke; Zhang, Xiao-Yan; Zhang, Zhe; Gou, Xue-Ya; Ding, Ya-Nan; Li, Qiao; Liang, Yong-Min published the article 《Palladium-Catalyzed C-H Amination/[2+3] or [2+4] Cyclization via C(sp3 or sp2)-H Activation》 about this compound( cas:4045-24-3 ) in Organic Letters. Keywords: amino fused bicyclic compound preparation regioselective; iodoarene benzoyloxyamine norbornadiene Catellani reaction amination cyclization palladium catalyst. Let’s learn more about this compound (cas:4045-24-3).

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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Pyrroline – Wikipedia,
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Wu, Peng; Huang, Wei; Cheng, Tai-Jin; Lin, Hai-Xia; Xu, Hui; Dai, Hui-Xiong published an article about the compound: 4-Methoxypiperidine( cas:4045-24-3,SMILESS:COC1CCNCC1 ).Safety of 4-Methoxypiperidine. 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.

A copper-catalyzed oxalamide-directed ortho-C-H amination of anilines has been developed by using 1 atm of air as the sole oxidant. The protocol shows excellent functional group tolerance, and some heterocyclic amines including indole, benzothiophene, benzothiazole, quinoline, isoquinoline, and quinoxaline could be compatible in the reaction. The late-stage diversification of medicinal drugs demonstrates the synthetic utility of this protocol.

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Pyrroline – Wikipedia,
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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.Electric Literature of C9H9ClN2. The article 《Electrochemical Iodoamination of Indoles Using Unactivated Amines》 in relation to this compound, is published in Organic Letters. Let’s take a look at the latest research on this compound (cas:4045-24-3).

An environmentally friendly electrochem. approach for iodoamination of various indole derivatives with a series of unactivated amines, amino acid derivatives, and benzotriazoles (more than 80 examples) has been developed. This strategy was further applied in late-stage functionalization of natural products and pharmaceuticals and gram-scale synthesis and radiosynthesis of 131I-labeled compounds Fundamental insights into the mechanism of the reaction based on control experiments, d. functional theory calculation, and cyclic voltammetry are provided.

Compound(4045-24-3)COA of Formula: C6H13NO received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(4-Methoxypiperidine), if you are interested, you can check out my other related articles.

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Pyrroline – Wikipedia,
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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.Product Details of 56413-95-7. The article 《Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:4045-24-3).

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.

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Pyrroline – Wikipedia,
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Formula: C6H13NO. 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: 4-Methoxypiperidine, is researched, Molecular C6H13NO, CAS is 4045-24-3, about Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.

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.

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Pyrroline – Wikipedia,
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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 Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors, published in 2021-01-01, which mentions a compound: 4045-24-3, Name is 4-Methoxypiperidine, Molecular C6H13NO, Reference of 4-Methoxypiperidine.

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.

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Pyrroline – Wikipedia,
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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: 4045-24-3, is researched, SMILESS is COC1CCNCC1, Molecular C6H13NOJournal, Article, Bioorganic & Medicinal Chemistry Letters called Orally bioavailable HCV NS5A inhibitors of unsymmetrical structural class, Author is Nakamura, Hiroshi; Fujioka, Shingo; Terui, Takashi; Okuda, Satoshi; Kondo, Kentaro; Tamatani, Yoshinori; Akagi, Yusuke; Komoda, Yasumasa; Kinoshita, Wataru; Ito, Soichiro; Maeda, Kimiya; Ukaji, Yutaka; Inaba, Takashi, the main research direction is bioavailability HCV NS5A inhibitor solubility permeability; Antiviral; HCV; NS5A; Oral bioavailability; Unsynmmetrical structure.Product Details of 4045-24-3.

A novel unsym. structural class of orally bioavailable hepatitis C virus (HCV) nonstructural 5A protein (NS5A) inhibitors has been generated by improving both the solubility and membrane permeability of the lead compound found in our previous work. The representative compound 14, with a 5-hydroxymethylpyrazine group and a 3-t-butylpropargyl group on each side of the mol., exhibited the best oral bioavailability in this study, inhibiting not only the HCV genotype 1a, 1b, 2a, and 3a replicons with EC50 values in the picomolar range, but also inhibited 1a Q30 mutants induced by launched sym. inhibitors with EC50 values in the low nanomolar range.

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Pyrroline – Wikipedia,
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Wang, Jin-Lin; Liu, Mei-Ling; Zou, Jian-Yu; Sun, Wen-Hui; Liu, Xue-Yuan published an article about the compound: 4-Methoxypiperidine( cas:4045-24-3,SMILESS:COC1CCNCC1 ).Product Details 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.

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.

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Pyrroline – Wikipedia,
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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 Orally bioavailable HCV NS5A inhibitors of unsymmetrical structural class, the main research direction is bioavailability HCV NS5A inhibitor solubility permeability; Antiviral; HCV; NS5A; Oral bioavailability; Unsynmmetrical structure.Product Details of 4045-24-3.

A novel unsym. structural class of orally bioavailable hepatitis C virus (HCV) nonstructural 5A protein (NS5A) inhibitors has been generated by improving both the solubility and membrane permeability of the lead compound found in our previous work. The representative compound 14, with a 5-hydroxymethylpyrazine group and a 3-t-butylpropargyl group on each side of the mol., exhibited the best oral bioavailability in this study, inhibiting not only the HCV genotype 1a, 1b, 2a, and 3a replicons with EC50 values in the picomolar range, but also inhibited 1a Q30 mutants induced by launched sym. inhibitors with EC50 values in the low nanomolar range.

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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 new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors, published in 2021-01-01, which mentions a compound: 4045-24-3, Name is 4-Methoxypiperidine, Molecular C6H13NO, COA of Formula: C6H13NO.

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.

From this literature《Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors》,we know some information about this compound(4045-24-3)COA of Formula: C6H13NO, but this is not all information, there are many literatures related to this compound(4045-24-3).

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