Tag: M.W=100-150

In 2019 ORG LETT published article about ASYMMETRIC MANNICH REACTION; ALDOL-TYPE REACTION; ENANTIOSELECTIVE SYNTHESIS; BRONSTED ACID; ETHYL DIAZOACETATE; ALPHA-DIAZOMETHYLPHOSPHONATES; 3-SUBSTITUTED ISOINDOLINONES; ARYLATION; ALDEHYDES; CASCADE in [Ray, Sumit K.; Sadhu, Milon M.; Biswas, Rayhan G.; Unhale, Rajshekhar A.] Indian Inst Sci Educ & Res Bhopal, Dept Chem, Bhopal 462066, MP, India; [Singh, Vinod K.] Indian Inst Technol Kanpur, Dept Chem, Kanpur 208016, Uttar Pradesh, India in 2019, Cited 93. 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

Chiral Bronsted acid catalyzed enantioselective syntheses of isoindolinones and phthalides have been accomplished via tandem Mannich-lactamization and aldol-lactonization reactions, respectively. A variety of enantioenriched isoindolinones (up to 99% ee) and phthalides (up to 85% ee) containing alpha-diazoesters were afforded in excellent yields. Furthermore, a concise synthesis of (S)-PD 172938 has been demonstrated by using this protocol.

Category: piperidines. Welcome to talk about 177-11-7, If you have any questions, you can contact Ray, SK; Sadhu, MM; Biswas, RG; Unhale, RA; Singh, VK or send Email.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

I found the field of Chemistry very interesting. Saw the article Site-Selective C-H Functionalization-Sulfination Sequence to Access Aryl Sulfonamides published in 2020. Safety of 1,4-Dioxa-8-azaspiro[4.5]decane, Reprint Addresses Ritter, T (corresponding author), Max Planck Inst Kohlenforsch, D-45470 Mulheim, Germany.. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 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.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Product Details of 177-11-7. Authors Sahoo, T; Sarkar, S; Ghosh, SC in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Sahoo, Tapan; Sarkar, Souvik; Ghosh, Subhash Chandra] Cent Salt & Marine Chem Res Inst CSIR CSMCRI, Nat Prod & Green Chem Div, GB Marg, Bhavnagar 364002, Gujarat, India; [Sahoo, Tapan; Ghosh, Subhash Chandra] Acad Sci & Innovat Res AcSIR, Ghaziabad 201002, India in 2021, Cited 50. 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 simple and facile copper(II) mediated protocol for C-8 amination of 1-naphthylamide derivatives is reported here. Picolinamide and its derivatives were used as a bidentate directing group for the C-8 amination reaction. Various substituted naphthylamide derivatives with numerous cyclic and acyclic amines proceed in good yields under mild conditions. Air was used solely as an oxidant. (C) 2021 Elsevier Ltd. All rights reserved.

Welcome to talk about 177-11-7, If you have any questions, you can contact Sahoo, T; Sarkar, S; Ghosh, SC or send Email.. Product Details of 177-11-7

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

In 2020 ORG LETT 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. Recommanded Product: 177-11-7

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.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

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. Safety of 1,4-Dioxa-8-azaspiro[4.5]decane

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.

Welcome to talk about 177-11-7, 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 send Email.. Safety of 1,4-Dioxa-8-azaspiro[4.5]decane

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Quality Control of 1,4-Dioxa-8-azaspiro[4.5]decane. Flood, DT; Zhang, XJ; Fu, X; Zhao, ZX; Asai, S; Sanchez, BB; Sturgell, EJ; Vantourout, JC; Richardson, P; Flanagan, ME; Piotrowski, DW; Kolmel, DK; Wan, JQ; Tsai, MH; Chen, JSS; Baran, PS; Dawson, PE in [Flood, Dillon T.; Zhang, Xuejing; Fu, Xiang; Zhao, Zhenxiang; Vantourout, Julien C.; Baran, Phil S.; Dawson, Philip E.] Scripps Res, Dept Chem, 10550 N Torrey Pines Rd, La Jolla, CA 92037 USA; [Zhang, Xuejing; Fu, Xiang] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Peoples R China; [Asai, Shota] Iwate Univ, Dept Chem & Biol Sci, Fac Engn, 4-3-5 Ueda, Morioka, Iwate 0208551, Japan; [Sanchez, Brittany B.; Sturgell, Emily J.; Chen, Jason S.] Scripps Res Inst, Automated Synth Facil, 10550 N Torrey Pines Rd, La Jolla, CA 92037 USA; [Richardson, Paul] Pfizer, Med Chem, 10770 Sci Ctr Dr, San Diego, CA 92121 USA; [Flanagan, Mark E.; Piotrowski, David W.; Kolmel, Dominik K.] Pfizer, Med Chem, Eastern Point Rd, Groton, CT 06340 USA; [Wan, Jinqiao; Tsai, Mei-Hsuan] HitGen Inc, Bldg 6,8 Huigu 1st East Rd Tianfu Int Bio Town, Chengdu 610200, Sichuan, Peoples R China published RASS-Enabled S/P-C and S-N Bond Formation for DEL Synthesis in 2020, Cited 49. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

DNA encoded libraries (DEL) have shown promise as a valuable technology for democratizing the hit discovery process. Although DEL provides relatively inexpensive access to libraries of unprecedented size, their production has been hampered by the idiosyncratic needs of the encoding DNA tag relegating DEL compatible chemistry to dilute aqueous environments. Recently reversible adsorption to solid support (RASS) has been demonstrated as a promising method to expand DEL reactivity using standard organic synthesis protocols. Here we demonstrate a suite of on-DNA chemistries to incorporate medicinally relevant and C-S, C-P and N-S linkages into DELs, which are underrepresented in the canonical methods.

Quality Control of 1,4-Dioxa-8-azaspiro[4.5]decane. Welcome to talk about 177-11-7, If you have any questions, you can contact Flood, DT; Zhang, XJ; Fu, X; Zhao, ZX; Asai, S; Sanchez, BB; Sturgell, EJ; Vantourout, JC; Richardson, P; Flanagan, ME; Piotrowski, DW; Kolmel, DK; Wan, JQ; Tsai, MH; Chen, JSS; Baran, PS; Dawson, PE or send Email.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

I found the field of Chemistry very interesting. Saw the article SYNTHESIS AND ANTITUBERCULAR EVALUATION OF FLUORINATED 2-CYCLOALKYLIMINO SUBSTITUTED 1,3-BENZOTHIAZIN-4-ONES published in 2019. Name: 1,4-Dioxa-8-azaspiro[4.5]decane, Reprint Addresses Nosova, EV (corresponding author), Ural Fed Univ, Dept Organ & Biomol Chem, 19 Mira st, Ekaterinburg 620002, Russia.; Nosova, EV (corresponding author), Russian Acad Sci, Postovsky Inst Organ Synth, Ural Branch, 22 S Kovalevskaya St,20 Akad Skaya St, Ekaterinburg 620137, Russia.. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane

Novel fluorinated 2-substituted 1,3-benzothiazin-4-ones were obtained through the addition of N-nucleophiles to ortho-fluorobenzoylisothiocyanates, followed by cyclization of fluorobenzoyl-thioureas. Synthetic approaches to original 2-cycloalkylimino- and 2-carbonylpiperazino- substituted benzothiazinones, bearing different number of fluorine atoms in the benzene ring have been found. 2-Ethoxycarbonylpiperazino-5-fluoro-1,3-benzothiazin-4-one proved to exhibit a high tuberculostatic activity in vitro (MIC 0.7 microgram/mL), thus indicating that a search of biologically active compounds in this family of heterocycles appears to be a reasonable approach.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Application In Synthesis of 1,4-Dioxa-8-azaspiro[4.5]decane. Kopruluoglu, C; Dejmek, M; Sala, M; Ajani, H; Hrebabecky, H; Fanfrlik, J; Jorda, R; Dracinsky, M; Prochazkova, E; Sacha, P; Krystof, V; Hobza, P; Lepsik, M; Nencka, R 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 published Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors in 2020, Cited 45. 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.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

An article Direct Catalytic Reductive N-Alkylation of Amines with Carboxylic Acids: Chemoselective Enannine Formation and further Functionalizations WOS:000480503700099 published article about TERTIARY AMIDES; HYDROGENATION; DERIVATIVES; AMINATION; NITRILES; HYDROSILANES; METHYLATION; AMIDATION; CHEMISTRY; MECHANISM in [Trillo, Paz; Adolfsson, Hans] Umea Univ, Dept Chem, KBC3,Linnaeus Vag 10, SE-90187 Umea, Sweden in 2019, Cited 66. Product Details of 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

Direct reductive N-alkylation of secondary amines with carboxylic acids using molybdenum hexacarbonyl (5 mol %) as catalyst and diethoxymethylsilane as reducing agent generate enamines in a straightforward fashion in high yields. The formed enamines are without the need for isolation or purification further reacted with trimethylsilyl cyanide in the same reaction flask to yield alpha-amino nitriles in good yields. In the optimized reaction conditions equimolar amounts of carboxylic acid and amine are reacted under neat conditions, and a catalytic amount of trifluoroethanol (0.1 mol %) is added along with TMSCN for the cyanation step. The reductive N-alkylation reaction is demonstrated to be highly chemoselective, tolerating a multitude of different functional groups present in the starting carboxylic acids and amines. The reaction is scalable and the generated alpha-amino nitriles are converted to other useful compounds, e.g., alpha-amino acids or amino-tetrazoles. In addition, the intermediate enamines are further transformed into triazolines, sulfonylformamidines, pyrimidinediones, and TMS-propargylamines, respectively, in high yields under mild reaction conditions. Benzoic acids react with secondary amines under similar conditions to give tertiary amines in high yields, and using this methodology, the biologically active compound Piribedil was isolated in 80% yield in a direct one-pot reaction setup.

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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.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem