Day: November 9, 2021

An article Diastereoselective synthesis of chiral 3-substituted isoindolinones via rhodium(iii)-catalyzed oxidative C-H olefination/annulation WOS:000661230200001 published article about N-ACYL KETIMINES; ASYMMETRIC-SYNTHESIS; ENANTIOSELECTIVE SYNTHESIS; 1,3-DISUBSTITUTED ISOINDOLINES; STEREOSELECTIVE-SYNTHESIS; CATALYZED ARYLATION; MICHAEL REACTIONS; DIRECTING GROUP; 3+2 ANNULATION; ACTIVATION in [Li, Xue-Hong; Gong, Jun-Fang; Song, Mao-Ping] Zhengzhou Univ, Green Catalysis Ctr, Coll Chem, Zhengzhou 450001, Peoples R China in 2021, Cited 104. Formula: C7H13NO2. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

A new method for the direct and stereoselective synthesis of 3-substituted isoindolinones via Rh(iii)-catalyzed chiral N-sulfinyl amide directed asymmetric [4 + 1] annulation of benzamides with acrylic esters has been developed. The reaction proceeded through an oxidative C-H olefination and a subsequent cyclization by intramolecular aza-Michael addition, producing a series of diastereoisomeric chiral isoindolinones (20 examples) in generally good yields with a dr value up to 5.5 : 1. The absolute configurations of the newly formed C-stereocenters in the major and minor diastereomers of the catalysis product have been determined by X-ray crystal diffraction analysis to be S and R, respectively. The separation of the major diastereoisomers from the catalysis products and subsequent removal of the N-sulfinyl chiral auxiliary afforded enantiomerically pure (S)-isoindolinones. The application of the obtained (S)-isoindolinones in the synthesis of several biologically active isoindolinones such as (S)-PD172938, (S)-pazinaclone and (S)-pagoclone is presented.

Formula: C7H13NO2. Welcome to talk about 177-11-7, If you have any questions, you can contact Li, XH; Gong, JF; Song, MP or send Email.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Authors Tan, YJ; Li, M; Gunawan, GA; Nyantakyi, SA; Dick, T; Go, ML; Lam, YL in AMER CHEMICAL SOC published article about BIOLOGICAL EVALUATION; MMPL3; INHIBITION in [Tan, Yu Jia; Gunawan, Gregory Adrian; Lam, Yulin] Natl Univ Singapore, Dept Chem, Singapore 117543, Singapore; [Li, Ming; Nyantakyi, Samuel Agyei; Go, Mei-Lin] Natl Univ Singapore, Dept Pharm, Singapore 117543, Singapore; [Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Hackensack Meridian Sch Med, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20057 USA in 2021, Cited 19. Formula: C7H13NO2. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here we found that modifying the incipient scaffold by amide-amine substitution and replacing the indole ring with benzothiophene or benzoselenophene led to striking (10-20-fold) improvements in solubility. Potent activity could be achieved without the carboxamide linker but not in the absence of the indole ring. The indolylmethylamine, N-cyclooctyl-6-trifluoromethylindol-2-ylmethylamine (33, MIC90Mtb , 0.13 mu M, MBC99.9Mtb, 0.63 mu M), exemplifies a promising member that is more soluble and equipotent to its carboxamide equivalent. It is also an inhibitor of the mycolate transporter MmpL3, a property shared by the methylamines of benzothiophene and benzoselenophene.

Formula: C7H13NO2. Bye, fridends, I hope you can learn more about C7H13NO2, If you have any questions, you can browse other blog as well. See you lster.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

An article Design, synthesis and biological evaluation of tetracyclic azafluorenone derivatives with topoisomerase I inhibitory properties as potential anticancer agents WOS:000504900300246 published article about RAPID COLORIMETRIC ASSAY; ANTIPROLIFERATIVE EVALUATION; MOLECULAR HYBRIDIZATION; ANALOGS; CANCER; CAMPTOTHECIN; ALKALOIDS; MECHANISM; DISCOVERY; APOPTOSIS in [Chen, Tsung-Chih; Chen, Chun-Liang; Lee, Chia-Chung; Huang, Hsu-Shan] Taipei Med Univ, Coll Med Sci & Technol, Grad Inst Canc Biol & Drug Discovery, Taipei 110, Taiwan; [Chen, Tsung-Chih; Yu, Dah-Shyong; Chen, Chun-Liang; Lee, Chia-Chung; Huang, Hsu-Shan] Natl Def Med Ctr, Grad Inst Life Sci, Taipei 114, Taiwan; [Chen, Tsung-Chih; Chen, Shiag-Jiun; Hsieh, Ying-Yu; Huang, Hsu-Shan] Natl Def Med Ctr, Sch Pharm, Taipei 114, Taiwan; [Yu, Dah-Shyong] Triserv Gen Hosp, Dept Surg, Div Urol, Urooncol Lab, Taipei 114, Taiwan; [Yu, Dah-Shyong] Natl Def Med Ctr, Inst Prevent Med, Taipei 114, Taiwan; [Chang, Lien-Cheng; Lin, Jing-Jer] Natl Taiwan Univ, Coll Med, Inst Biochem & Mol Biol, Taipei 100, Taiwan; [Chang, Lien-Cheng] Minist Hlth & Welf, Food & Drug Adm, Taipei 115, Taiwan; [Guh, Jih-Hwa] Natl Taiwan Univ, Sch Pharm, Taipei 100, Taiwan in 2019, Cited 40. Recommanded Product: 177-11-7. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

Several 9-chloro-11H-indeno[1,2-c]quinolin-11-one derivatives have been designed which is replacing side chains with different groups containing oxygen, nitrogen or sulfur atoms. Substitution of C-6 on the starting structure, 6,9-dichloro-11H-indeno[1,2-c]quinolin-11-one, using apposite nucleophilic group with a suitable base or acid could be obtained 28 novel tetracyclic azafluorenone derivatives. The cytotoxic activity of these analogues was examined in cancer cell lines by MTT assay and compounds 4, 5, 13, and 26 were selected to evaluate in topoisomerase I drug screening assay, respectively. At the same time, 17 compounds were selected for NCI-60 anticancer drug screen to prevent the narrower concept of an in vitro screening model. Its worth to find that 9-chloro-6-(piperazin-1-yl)-11H-indeno[1,2-c]quinolin-11-one (12) showed greater cytotoxicity than another azafluorenone derivatives with an average GI(50) of 10.498 mu M over 60 cell lines. We also found that another analogue, 9-chloro-6-(2-methylpiperazin-1-yl)-11H-indeno[1,2-c]quinolin-11-one (13), exhibited preferential growth inhibition effect toward cancer cell lines and showed a significant inhibitory effect on topoisomerase I. (C) 2016 Production and hosting by Elsevier B.V. on behalf of King Saud University.

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Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. Recently I am researching about SULFONYL FLUORIDES; CLICK CHEMISTRY; TOSYLATES; CHLORIDES; REAGENT, Saw an article supported by the National Institute of General Medical Sciences of the National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R15GM134457]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Mahapatra, S; Woroch, CP; Butler, TW; Carneiro, SN; Kwan, SC; Khasnavis, SR; Gu, J; Dutra, JK; Vetelino, BC; Bellenger, J; Ende, CWA; Ball, ND. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane

A method to activate sulfamoyl fluorides, fluorosulfates, and sulfonyl fluorides with calcium triflimide and DABCO for SuFEx with amines is described. The reaction was applied to a diverse set of sulfamides, sulfamates, and sulfonamides at room temperature under mild conditions. Additionally, we highlight this transformation to parallel medicinal chemistry to generate a broad array of nitrogen-based S(VI) compounds.

Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. Welcome to talk about 177-11-7, If you have any questions, you can contact Mahapatra, S; Woroch, CP; Butler, TW; Carneiro, SN; Kwan, SC; Khasnavis, SR; Gu, J; Dutra, JK; Vetelino, BC; Bellenger, J; Ende, CWA; Ball, ND or send Email.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Product Details of 177-11-7. Di Mussi, R; Spadaro, S; Volta, CA; Bartolomeo, N; Trerotoli, P; Staffieri, F; Pisani, L; Iannuzziello, R; Dalfino, L; Murgolo, F; Grasso, S in [Di Mussi, Rosa; Pisani, Luigi; Iannuzziello, Rachele; Dalfino, Lidia; Murgolo, Francesco; Grasso, Salvatore] Univ Bari Aldo Moro, Osped Policlin, Dipartimento Emergenza & Trapianti Organo DETO, Sez Anestesiol & Rianimaz, Piazza Giulio Cesare 11, Bari, Italy; [Spadaro, Savino; Volta, Carlo Alberto] Univ Ferrara, Dipartimento Morfol Chirurg & Med Sperimentale, Sez Anestesiol & Terapia Intens Univ, Ferrara, Italy; [Bartolomeo, Nicola; Trerotoli, Paolo] Univ Aldo Moro, Dipartimento Sci Biomed & Oncol Umana, Cattedra Stat Med, Bari, Italy; [Staffieri, Francesco] Univ Bari Aldo Moro, Dipartimento Emergenza & Trapianti Organo DETO, Sez Chirurg Vet, Bari, Italy published Continuous assessment of neuro-ventilatory drive during 12 h of pressure support ventilation in critically ill patients in 2020, Cited 67. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

Introduction Pressure support ventilation (PSV) should allow spontaneous breathing with a normal neuro-ventilatory drive. Low neuro-ventilatory drive puts the patient at risk of diaphragmatic atrophy while high neuro-ventilatory drive may causes dyspnea and patient self-inflicted lung injury. We continuously assessed for 12 h the electrical activity of the diaphragm (EAdi), a close surrogate of neuro-ventilatory drive, during PSV. Our aim was to document the EAdi trend and the occurrence of periods of Low and/or High neuro-ventilatory drive during clinical application of PSV. Method In 16 critically ill patients ventilated in the PSV mode for clinical reasons, inspiratory peak EAdi peak (EAdi(PEAK)), pressure time product of the trans-diaphragmatic pressure per breath and per minute (PTPDI/b and PTPDI/min, respectively), breathing pattern and major asynchronies were continuously monitored for 12 h (from 8 a.m. to 8 p.m.). We identified breaths with Normal (EAdi(PEAK) 5-15 mu V), Low (EAdi(PEAK) < 5 mu V) and High (EAdi(PEAK) > 15 mu V) neuro-ventilatory drive. Results Within all the analyzed breaths (177.117), the neuro-ventilatory drive, as expressed by the EAdi(PEAK), was Low in 50.116 breath (28%), Normal in 88.419 breaths (50%) and High in 38.582 breaths (22%). The average times spent in Low, Normal and High class were 1.37, 3.67 and 0.55 h, respectively (p < 0.0001), with wide variations among patients. Eleven patients remained in the Low neuro-ventilatory drive class for more than 1 h, median 6.1 [3.9-8.5] h and 6 in the High neuro-ventilatory drive class, median 3.4 [2.2-7.8] h. The asynchrony index was significantly higher in the Low neuro-ventilatory class, mainly because of a higher number of missed efforts. Conclusions We observed wide variations in EAdi amplitude and unevenly distributed Low and High neuro ventilatory drive periods during 12 h of PSV in critically ill patients. Further studies are needed to assess the possible clinical implications of our physiological findings. Welcome to talk about 177-11-7, If you have any questions, you can contact Di Mussi, R; Spadaro, S; Volta, CA; Bartolomeo, N; Trerotoli, P; Staffieri, F; Pisani, L; Iannuzziello, R; Dalfino, L; Murgolo, F; Grasso, S or send Email.. Product Details of 177-11-7

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Li, XJ; Payne, DT; Ampolu, B; Bland, N; Brown, JT; Dutton, MJ; Fitton, CA; Gulliver, A; Hale, L; Hamza, D; Jones, G; Lane, R; Leach, AG; Male, L; Merisor, EG; Morton, MJ; Quy, AS; Roberts, R; Scarll, R; Schulz-Utermoehl, T; Stankovic, T; Stevenson, B; Fossey, JS; Agathanggelou, A in [Li, Xingjian; Payne, Daniel T.; Dutton, Mark J.; Quy, Alex S.; Fossey, John S.] Univ Birmingham, Sch Chem, Birmingham B15 2TT, W Midlands, England; [Ampolu, Badarinath; Bland, Nicholas; Brown, Jane T.; Hamza, Daniel; Jones, Geraint; Lane, Rebecca; Merisor, Elena G.; Schulz-Utermoehl, Timothy; Stevenson, Brett] BioCity, Sygnat Discovery, Discovery Bldg,Pennyfoot St, Nottingham NG1 1GR, England; [Fitton, Catherine A.; Scarll, Rosanna; Stankovic, Tatjana; Agathanggelou, Angelo] Univ Birmingham, Inst Canc & Genom Sci, Birmingham B15 2TT, W Midlands, England; [Gulliver, Abigail; Hale, Lee] Univ Birmingham, Winterbourne Bot Garden, 58 Edgbaston Pk Rd, Birmingham B15 2RT, W Midlands, England; [Leach, Andrew G.] Liverpool John Moores Univ, Sch Pharm & Biomol Sci, Byrom St, Liverpool L3 3AF, Merseyside, England; [Male, Louise] Univ Birmingham, Sch Chem, Xray Crystallog Facil, Birmingham B15 2TT, W Midlands, England; [Morton, Michael J.; Roberts, Ruth] ApconiX Ltd, Alderly Pk, Nether Alderly SK10 4TG, Cheshire, England; [Roberts, Ruth] Univ Birmingham, Sch Biosci, Birmingham B15 2TT, W Midlands, England published Derivatisation of parthenolide to address chemoresistant chronic lymphocytic leukaemia in 2019, Cited 143. COA of Formula: C7H13NO2. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

Parthenolide is a natural product that exhibits anti-leukaemic activity, however, its clinical use is limited by its poor bioavailability. It may be extracted from feverfew and protocols for growing, extracting and derivatising it are reported. A novel parthenolide derivative with good bioavailability and pharmacological properties was identified through a screening cascade based on in vitro anti-leukaemic activity and calculated drug-likeness properties, in vitro and in vivo pharmacokinetics studies and hERG liability testing. In vitro studies showed the most promising derivative to have comparable anti-leukaemic activity to DMAPT, a previously described parthenolide derivative. The newly identified compound was shown to have pro-oxidant activity and in silico molecular docking studies indicate a prodrug mode of action. A synthesis scheme is presented for the production of amine 7 used in the generation of 5f.

COA of Formula: C7H13NO2. Bye, fridends, I hope you can learn more about C7H13NO2, If you have any questions, you can browse other blog as well. See you lster.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Recently I am researching about ANTI-MARKOVNIKOV HYDROAMINATION; INTERMOLECULAR HYDROAMINATION; ALKENES; DISCOVERY; ALDEHYDES, Saw an article supported by the NIHUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USA [R35 GM125029]; Sloan FoundationAlfred P. Sloan Foundation [FG-2016-6568]; University of Illinois; NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R35GM125029] Funding Source: NIH RePORTER. Product Details of 177-11-7. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Vanable, EP; Kennemur, JL; Joyce, LA; Ruck, RT; Schultz, DM; Hull, KL. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane

A Rh-catalyzed enantioselective hydroamination of allylamines using a chiral BIPHEP-type ligand is reported. Enantioenriched 1,2-diamines are formed in good yields and with excellent enantioselectivities. A diverse array of nucleophiles and amine directing groups are demonstrated, including deprotectable motifs. Finally, the methodology was demonstrated toward the rapid synthesis of 2-methyl-moclobemide.

Product Details of 177-11-7. Welcome to talk about 177-11-7, If you have any questions, you can contact Vanable, EP; Kennemur, JL; Joyce, LA; Ruck, RT; Schultz, DM; Hull, KL or send Email.

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Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

An article Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors WOS:000549952000002 published article about SCORING FUNCTION; SMALL MOLECULES; ROSCOVITINE; POTENT; IDENTIFICATION; SITE in [Kopruluoglu, Cemal; Dejmek, Milan; Sala, Michal; Ajani, Haresh; Hrebabecky, Hubert; Fanfrlik, Jindrich; Dracinsky, Martin; Prochazkova, Eliska; Sacha, Pavel; Hobza, Pavel; Lepsik, Martin; Nencka, Radim] Czech Acad Sci, Inst Organ Chem & Biochem, Flemingovo Nam 2, Prague 16610 6, Czech Republic; [Kopruluoglu, Cemal; Ajani, Haresh; Hobza, Pavel] Palacky Univ, Reg Ctr Adv Technol & Mat, Dept Phys Chem, Olomouc, Czech Republic; [Jorda, Radek; Krystof, Vladimir] Palacky Univ, Fac Sci, Lab Growth Regulators, Olomouc, Czech Republic; [Jorda, Radek; Krystof, Vladimir] Czech Acad Sci, Inst Expt Bot, Olomouc, Czech Republic in 2020, Cited 45. Formula: C7H13NO2. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7

We report on the discovery of norbornyl moiety as a novel structural motif for cyclin-dependent kinase 2 (CDK2) inhibitors which was identified by screening a carbocyclic nucleoside analogue library. Three micromolar hits were expanded by the use of medicinal chemistry methods into a series of 16 novel compounds. They had prevailingly micromolar activities against CDK2 and the best compound of the series attained IC(50)of 190 nM. The binding modes were explored in molecular details by modeling and docking. Quantum mechanics-based scoring was used to rationalize the affinities. In conclusion, the discovered 9-hydroxymethylnorbornyl moiety was shown by joint experimental-theoretical efforts to be able to serve as a novel substituent for CDK2 inhibitors. This finding opens door to the exploration of chemical space towards more effective derivatives targeting this important class of protein kinases.

Formula: C7H13NO2. Bye, fridends, I hope you can learn more about C7H13NO2, If you have any questions, you can browse other blog as well. See you lster.

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Piperidine – Wikipedia,
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I found the field of Chemistry very interesting. Saw the article Iron-catalyzed regioselective alkylation of 1,4-quinones and coumarins with functionalized alkyl bromides published in 2020. SDS of cas: 177-11-7, Reprint Addresses Li, DK (corresponding author), Qujing Normal Univ, Coll Chem & Environm Sci, Qujing 655011, Yunnan, Peoples R China.; Shen, XF (corresponding author), Qujing Normal Univ, Ctr Yunnan Guizhou Plateau Chem Funct Mat & Pollu, Qujing 655011, Yunnan, Peoples R China.. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane

A simple and efficient Fe-catalyzed regioselective alkylation of 1,4-quinones and coumarins, using functionalized alkyl bromides as alkylating reagents, has been developed. The reaction proceeds under mild conditions with the addition of alkyl bromides to a wide range of 1,4-quinone and coumarin derivatives with a broad substrate scope and wide functional group tolerance to provide the products in good yields. Further application of these strategies could be extended to important biologically active antimalarial lead drugs, such as plasmodione on a gram scale in a single step for medicinal purposes.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

In 2021 ACS MED CHEM LETT published article about BIOLOGICAL EVALUATION; MMPL3; INHIBITION in [Tan, Yu Jia; Gunawan, Gregory Adrian; Lam, Yulin] Natl Univ Singapore, Dept Chem, Singapore 117543, Singapore; [Li, Ming; Nyantakyi, Samuel Agyei; Go, Mei-Lin] Natl Univ Singapore, Dept Pharm, Singapore 117543, Singapore; [Dick, Thomas] Hackensack Meridian Hlth, Ctr Discovery & Innovat, Hackensack Meridian Sch Med, Nutley, NJ 07110 USA; [Dick, Thomas] Georgetown Univ, Dept Microbiol & Immunol, Washington, DC 20057 USA in 2021, Cited 19. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Recommanded Product: 1,4-Dioxa-8-azaspiro[4.5]decane

Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here we found that modifying the incipient scaffold by amide-amine substitution and replacing the indole ring with benzothiophene or benzoselenophene led to striking (10-20-fold) improvements in solubility. Potent activity could be achieved without the carboxamide linker but not in the absence of the indole ring. The indolylmethylamine, N-cyclooctyl-6-trifluoromethylindol-2-ylmethylamine (33, MIC90Mtb , 0.13 mu M, MBC99.9Mtb, 0.63 mu M), exemplifies a promising member that is more soluble and equipotent to its carboxamide equivalent. It is also an inhibitor of the mycolate transporter MmpL3, a property shared by the methylamines of benzothiophene and benzoselenophene.

Recommanded Product: 1,4-Dioxa-8-azaspiro[4.5]decane. Welcome to talk about 177-11-7, If you have any questions, you can contact Tan, YJ; Li, M; Gunawan, GA; Nyantakyi, SA; Dick, T; Go, ML; Lam, YL or send Email.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem