Month: October 2021

An article Site-Selective C-H Functionalization-Sulfination Sequence to Access Aryl Sulfonamides WOS:000543669800003 published article about PALLADIUM-CATALYZED SYNTHESIS; SULFUR-DIOXIDE SURROGATE; ONE-POT; SULFONYL FLUORIDES; BORONIC ACIDS; DABSO; BORYLATION; RONGALITE; REAGENTS; HALIDES in [Alvarez, Eva Maria; Plutschack, Matthew B.; Berger, Florian; Ritter, Tobias] Max Planck Inst Kohlenforsch, D-45470 Mulheim, Germany in 2020, Cited 33. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Name: 1,4-Dioxa-8-azaspiro[4.5]decane

Aryl sulfinates are precursors to a diverse number of sulfonyl-derived arenes, which are common motifs in pharmaceuticals and agrochemicals. Here, we report a site-selective two-step C-H sulfination sequence via aryl sulfonium salts to access aryl sulfonamides. Combined with site-selective aromatic thianthrenation, an operationally simple one-pot palladium-catalyzed protocol introduces the sulfonyl group using sodium hydroxymethylsulfinate (Rongalite) as a source of SO22-. The hydroxymethyl sulfone intermediate generated from the catalytic process can be employed as a synthetic handle to deliver a variety of sulfonyl-containing compounds.

Name: 1,4-Dioxa-8-azaspiro[4.5]decane. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Alvarez, EM; Plutschack, MB; Berger, F; Ritter, T or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

COA of Formula: C7H13NO2. In 2020 ORG LETT published article about CATALYZED FLUOROSULFONYLVINYLATION; ARYLETHENESULFONYL FLUORIDES; ETHENESULFONYL FLUORIDE; LEAVING GROUPS; DUAL WARHEAD; HYDROAMINATION; INHIBITORS; CHEMISTRY; MACROLIDES; RESISTANCE in [Leng, Jing; Fang, Wan-Yin; Zhao, Chuang; Qin, Hua-Li] Wuhan Univ Technol, State Key Lab Silicate Mat Architectures, Wuhan 430070, Peoples R China; [Leng, Jing; Fang, Wan-Yin; Zhao, Chuang; Qin, Hua-Li] Wuhan Univ Technol, Sch Chem Chem Engn & Life Sci, Wuhan 430070, Peoples R China; [Tang, Wenjian] Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China in 2020, Cited 52. 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 clickable connective hub 1-bromo-2-triazole-thane-1-sulfonyl fluoride BTESF (1) was developed and successfully applied for the fluorosulfonylvinylation of a host of primary and secondary cyclic or acyclic amines including amino acids and pharmaceuticals. Further antimicrobial experiments revealed that vinyl sulfonyl fluoride functionalized norfloxacin (3ak), ciprofloxacin (3am), and lomefloxacin (3an) exhibited 4-fold improved antimicrobial activity against Gram-positive bacteria compared to their parent drugs.

COA of Formula: C7H13NO2. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Leng, J; Tang, WJ; Fang, WY; Zhao, C; Qin, HL or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Authors Elagamy, A; Althagafi, I; Pratap, R in ROYAL SOC CHEMISTRY published article about STEREOSELECTIVE-SYNTHESIS in [Elagamy, Amr; Pratap, Ramendra] Univ Delhi, Dept Chem, North Campus, Delhi 110007, India; [Althagafi, Ismail] Umm Al Qura Univ, Fac Sci, Chem Dept, Mecca 21955, Saudi Arabia in 2021, Cited 36. Quality Control of 1,4-Dioxa-8-azaspiro[4.5]decane. 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 mild and efficient route for the synthesis of conjugated trienes via nitroethane-mediated ring contraction of 2-oxobenzo[h]chromenes/2H-pyran-2-ones followed by decarboxylative rearrangement of the obtained spirobutenolides and butenolides is described. The (E)-isomer of trienes was obtained by step-wise and one-pot approaches from 2-oxobenzo[h]chromenes. Butenolides 4a-l as new substrates have been developed for the construction of trienes. The mixture of the (E)- and (Z)-isomers of spirobutenolides undergoes decarboxylative rearrangement in the presence of sodium ethoxide as a base to yield the (E)-isomer of trienes, while the (E)-isomer of butenolides reacts to give a mixture of (2E,4E)- and (2E,4Z)-isomers of trienes in an almost steady ratio of 45 : 55 or 1 : 1.2. The structure and geometry of the obtained butenolides and trienes were confirmed by single-crystal X-ray analysis.

Quality Control of 1,4-Dioxa-8-azaspiro[4.5]decane. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Elagamy, A; Althagafi, I; Pratap, R or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Name: 1,4-Dioxa-8-azaspiro[4.5]decane. In 2019 J MED CHEM published article about AGONIST SALVINORIN; PROLACTIN; DYNORPHIN; LY2456302; DOPAMINE; STRESS; 2-METHYL-N-((2′-(PYRROLIDIN-1-YLSULFONYL)BIPHENYL-4-YL)METHYL)PROPAN-1-AMINE; EXPRESSION; DISCOVERY; BINDING in [Guerrero, Miguel; Urbano, Mariangela; Kim, Eun-Kyong; Gamo, Ana M.; Riley, Sean; Abgaryan, Lusine; Leaf, Nora; Brown, Steven J.; Rosen, Hugh; Roberts, Edward] Scripps Res Inst, Dept Mol Med, 10550 North Torrey Pines Rd, La Jolla, CA 92037 USA; [Van Orden, Lori Jean] BlackThorn Therapeut Inc, 780 Brannan St, San Francisco, CA 94103 USA; [Xie, Jennifer Y.; Porreca, Frank] Univ Arizona, Dept Pharmacol, Tucson, AZ 85724 USA; [Cameron, Michael D.] Scripps Res Inst, Dept Mol Med, Jupiter, FL 33458 USA; [Xie, Jennifer Y.] Arkansas State Univ, Coll Osteopath Med, New York Inst Technol, Dept Basic Sci, Jonesboro, AR 72446 USA in 2019, Cited 47. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

kappa opioid receptor (KOR) antagonists are potential pharmacotherapies for the treatment of migraine and stress-related mood disorders including depression, anxiety, and drug abuse, thus the development of novel KOR antagonists with an improved potency/selectivity profile and medication-like duration of action has attracted the interest of the medicinal chemistry community. In this paper, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2 H-pyran-4-yl)piperidin-4 amine (CYM-53093, BTRX-335140) as a potent and selective KOR antagonist, endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments. Orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. This compound is in phase 1 clinical trials for the treatment of neuropsychiatric disorders wherein dynorphin is thought to contribute to the underlying pathophysiology.

Name: 1,4-Dioxa-8-azaspiro[4.5]decane. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Guerrero, M; Urbano, M; Kim, EK; Gamo, AM; Riley, S; Abgaryan, L; Leaf, N; Van Orden, LJ; Brown, SJ; Xie, JY; Porreca, F; Cameron, MD; Rosen, H; Roberts, E or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

An article Amide-Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility WOS:000651790900005 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. Application In Synthesis of 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.

About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Tan, YJ; Li, M; Gunawan, GA; Nyantakyi, SA; Dick, T; Go, ML; Lam, YL or concate me.. Application In Synthesis of 1,4-Dioxa-8-azaspiro[4.5]decane

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Recommanded Product: 177-11-7. 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.

Recommanded Product: 177-11-7. About 1,4-Dioxa-8-azaspiro[4.5]decane, 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 concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. In 2021 APPL ORGANOMET CHEM published article about PHOSPHORUS-NITROGEN COMPOUNDS; DNA INTERACTIONS; INTERMOLECULAR INTERACTIONS; BIOLOGICAL-ACTIVITIES; CRYSTAL-STRUCTURES; CHIRAL CONFIGURATIONS; QUANTITATIVE-ANALYSIS; HIRSHFELD SURFACES; CYCLOTRIPHOSPHAZENE; ANTITUBERCULOSIS in [Okumus, Aytug; Elmas, Gamze; Kilic, Zeynel] Ankara Univ, Dept Chem, Ankara, Turkey; [Binici, Arzu] Republ Turkey Minist Hlth, Ankara, Turkey; [Ramazanoglu, Nagehan] Sci & Technol Res Council Turkey, Ankara, Turkey; [Acik, Leyla] Gazi Univ, Dept Biol, Ankara, Turkey; [cosut, Bunyemin] Gebze Tech Univ, Dept Chem, Gebze, Turkey; [Hokelek, Tuncer] Hacettepe Univ, Dept Phys, Ankara, Turkey; [Guzel, Remziye] Dicle Univ, Dept Chem, Diyarbakir, Turkey; [Tunali, Beste cagdas; Turk, Mustafa] Kirikkale Univ, Dept Bioengn, Kirikkale, Turkey; [Simsek, Hulya] Bozok Univ, Dept Microbiol, Yozgat, Turkey in 2021, Cited 106. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

In this study, two kinds of compounds, namely, mono-ferrocenyl-2-cis-4-dichloro-ansa- (2,4-ansa; 3) and mono-ferrocenyl-spiro- (spiro; 4) hexachlorocyclotetraphosphazenes, were obtained by the Cl replacement reaction of N4P4Cl8 (1) with an equimolar amount of sodium 3-(N-ferrocenylmethylamino)-1-propanoxide (2). The reactions of 2,4-ansa (3) with excess diamines and dialkoxides resulted in the formation of ansa-cyclotetraphosphazenes (3a-3e). Spiro (4) was reacted with excess diamines and dialkoxides to give the mono-ferrocenyl-spiro-cyclotetraphosphazenes (4a-4d). Although 2,4-ansa (3) produced the dispiro (3a) with N-(4-fluorobenzyl)-N ‘-methylethane-1,2-diamine, it afforded both monospiro (3b) and dispiro (3c) with N-(4-fluorobenzyl)-N ‘-methylpropane-1,3-diamine. However, spiro (4) yielded a trispiro (4a) with N-(4-fluorobenzyl)-N ‘-methylethane-1,2-diamine and 2,6-dispiro (4b) with N-(4-fluorobenzyl)-N ‘-methylpropane-1,3-diamine. The structures of the phosphazenes were elucidated by FTIR, ESI-MS and/or HRMS, spectroscopic and crystallographic (for 3f and 4b) data. Furthermore, the electrochemical findings of cyclotetraphosphazenes exhibited electrochemically reversible one-electron oxidation of Fe-redox centre. As an example, the chirality of 3c was investigated by P-31 NMR spectroscopy on the addition of (R)-(+)-2,2,2-trifluoro-1-(9 ‘-anthryl)-ethanol, chiral solvating agent (CSA). The circular dichroism (CD) (for 3d and 3e), HPLC (for 3d, 3e and 3f) and X-ray (for 3f) display that these compounds have chirality (RS ‘ or SR ‘) in the solution and solid state. This paper also focuses on the antimicrobial activities, the interactions with pBR322 DNA, in vitro anticancer activity against L929 fibroblast and MCF7 breast cells, and antituberculosis activity against Mycobacterium tuberculosis H37Rv of the cyclotetraphosphazenes.

Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Okumus, A; Elmas, G; Kilic, Z; Binici, A; Ramazanoglu, N; Acik, L; Cosut, B; Hokelek, T; Guzel, R; Tunali, BC; Turk, M; Simsek, H or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

An article Amide-Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility WOS:000651790900005 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. Category: piperidines

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.

About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Tan, YJ; Li, M; Gunawan, GA; Nyantakyi, SA; Dick, T; Go, ML; Lam, YL or concate me.. Category: piperidines

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

I found the field of Chemistry very interesting. Saw the article Ni/NHC-catalyzed cross-coupling of methyl sulfinates and amines for direct access to sulfinamides published in 2019. Computed Properties of C7H13NO2, Reprint Addresses Chen, JZ (corresponding author), Zhejiang Univ, Coll Pharmaceut Sci, 866 Yuhangtang Rd, Hangzhou, Zhejiang, 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

It was reported to develop a simple and convenient method for the Ni/NHC-catalyzed cross-coupling of methyl sulfinates and amines without an acid/base to afford secondary or tertiary sulfinamides in moderate to good yields. The method can provide the desired products with broad substrate scope, good chemoselectivity and good functional group compatibility. The presented approach may enrich the Nil NHC catalyst system and promote the applications of methyl sulfinates in the organic sulfur chemistry. (C) 2019 Elsevier Ltd. All rights reserved.

Computed Properties of C7H13NO2. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Li, GJ; Pan, YL; Liu, YL; Xu, HF; Chen, JZ or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Zhang, BS; Li, YK; Gou, XY; Zhang, Z; An, Y; Wang, XG; Liang, YM in [Zhang, Bo-Sheng] Northwest Normal Univ, Coll Chem & Chem Engn, Lanzhou 730070, Gansu, Peoples R China; [Zhang, Bo-Sheng; Gou, Xue-Ya; Zhang, Zhe; An, Yang; Wang, Xin-Gang; Liang, Yong-Min] Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China; [Li, Yuke] Chinese Univ Hong Kong, Dept Chem, Shatin, Hong Kong, Peoples R China; [Li, Yuke] Chinese Univ Hong Kong, Ctr Sci Modeling & Computat, Shatin, Hong Kong, Peoples R China published DMAP and PivOH-promoted amination/allenization reaction in 2020, Cited 47. 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.

This report described the first DMAP and PivOH-promotedortho-C-H amination andipso-allenization reaction of iodobenzenes realized by Pd/norbornene cooperative catalysis. Based on control experiments and DFT calculations, we speculated that the three ligands have different functions and mechanism paths in the reaction.

About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Zhang, BS; Li, YK; Gou, XY; Zhang, Z; An, Y; Wang, XG; Liang, YM or concate me.. Formula: C7H13NO2

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem