Day: October 28, 2021

Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. Recently I am researching about ONE-POT SYNTHESIS; N-SULFONYLFORMAMIDINES; SULFONYL AMIDINES; TERTIARY-AMINES; METAL-FREE; INHIBITORS; DESIGN; ROUTE; INTERCEPTION; FORMAMIDINES, Saw an article supported by the Program of Young Talent Development in Yangtze Normal University [2018QNRC16]; Project for Basic Research and Frontier Exploration of Science and Technology Commission of Chongqing [cstc2019jcyjmsxml275, cstc2016jcyjA0056]; Science and Technology Research Program of the Chongqing Education Commission of China [KJQN201901422]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Gou, Q; Liu, ZN; Cao, TW; Tan, XP; Shi, WB; Ran, M; Cheng, FX; Qn, J. The CAS is 177-11-7. Through research, I have a further understanding and discovery of 1,4-Dioxa-8-azaspiro[4.5]decane

Herein, we describe an efficient copper-catalyzed coupling of sulfonamides with alkylamines to synthesize (E)-N-sulfonylformamidines. The reaction is accomplished under mild conditions without the use of a corrosive acid or base as an additive. It tolerates a broad scope of substrates and generates the products with exclusive (E)-stereoselectivity.

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 Gou, Q; Liu, ZN; Cao, TW; Tan, XP; Shi, WB; Ran, M; Cheng, FX; Qn, J or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

In 2021 ORG BIOMOL CHEM 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. 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

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.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Application In Synthesis of 1,4-Dioxa-8-azaspiro[4.5]decane. In 2020 J AM CHEM SOC published article about IN-VITRO; BENZENESULFINYL AZIDE; NH-SULFOXIMINES; CHEMISTRY; SUFEX; SULFUR; INHIBITOR; DISCOVERY; SULFIDES; SOF4 in [Davies, Thomas Q.; Tilby, Michael J.; Ren, Jack; Parker, Nicholas A.; Duarte, Fernanda; Willis, Michael C.] Univ Oxford, Dept Chem, Chem Res Lab, Oxford OX1 3TA, England; [Skolc, David; Hall, Adrian] UCB Biopharma SPRL, B-1420 Braine Lalleud, Belgium in 2020, Cited 68. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

Sulfoximines and sulfonimidamides are promising compounds for medicinal and agrochemistry. As monoaza analogues of sulfones and sulfonamides, respectively, they combine good physicochemical properties, high stability, and the ability to build complexity from a three-dimensional core. However, a lack of quick and efficient methods to prepare these compounds has hindered their uptake in molecule discovery programmes. Herein, we describe a unified, one-pot approach to both sulfoximines and sulfonimidamides, which exploits the high electrophilicity of sulfinyl nitrenes. We generate these rare reactive intermediates from a novel sulfinylhydroxylamine (R-O-N=S=O) reagent through an N-O bond fragmentation process. Combining sulfinyl nitrenes with carbon and nitrogen nucleophiles enables the synthesis of sulfoximines and sulfonimidamides in a reaction time of just 15 min. Alkyl, (hetero)aryl, and alkenyl organometallic reagents can all be used as the first or second component in the reaction, while primary and secondary amines, and anilines, all react with high efficiency as the second nucleophile. The tolerance of the reaction to steric and electronic factors has allowed for the synthesis of the most diverse set of sulfoximines and sulfonimidamides yet described. Experimental and computational investigations support the intermediacy of sulfinyl nitrenes, with nitrene formation proceeding via a transient triplet intermediate before reaching a planar singlet species.

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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. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. Formula: C7H13NO2

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.

Formula: C7H13NO2. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Trillo, P; Adolfsson, H or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

In 2019 J AM CHEM SOC published article about ANTI-MARKOVNIKOV HYDROAMINATION; INTERMOLECULAR HYDROAMINATION; ALKENES; DISCOVERY; ALDEHYDES in [Vanable, Evan P.; Kennemur, Jennifer L.; Hull, Kami L.] Univ Illinois, Dept Chem, 600 S Mathews, Urbana, IL 61801 USA; [Joyce, Leo A.; Ruck, Rebecca T.; Schultz, Danielle M.] Merck & Co Inc, Dept Proc Res & Dev, Rahway, NJ 07065 USA; [Kennemur, Jennifer L.] Max Planck Inst Kohlenforsch, Kaiser Wilhelm Pl 1, D-45470 Mulheim, Germany; [Hull, Kami L.] Univ Texas Austin, 105 E 24th St, Austin, TX 78712 USA in 2019, Cited 36. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7. COA of Formula: C7H13NO2

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.

COA of Formula: C7H13NO2. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Vanable, EP; Kennemur, JL; Joyce, LA; Ruck, RT; Schultz, DM; Hull, KL or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Authors Wei, MJ; Liang, DC; Cao, XH; Luo, WJ; Ma, GJ; Liu, ZY; Li, L in WILEY-V C H VERLAG GMBH published article about SUFEX CLICK CHEMISTRY; NUCLEOPHILIC-SUBSTITUTION; N-ALKYLATION; SULFONAMIDES; ARYL; DISCOVERY; AMINES; ARYLATION; PEPTIDES; REAGENTS in [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, PCFM Lab, Guangzhou 510275, Peoples R China; [Wei, Mingjie; Liang, Dacheng; Luo, Wenjun; Ma, Guojian; Liu, Zeyuan; Li, Le] Sun Yat Sen Univ, Sch Chem, GDHPRC Lab, Guangzhou 510275, Peoples R China; [Cao, Xiaohui] Guangdong Pharmaceut Univ, Sch Pharm, Guangzhou 510006, Peoples R China in 2021, Cited 144. Safety 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 broad-spectrum, catalytic method has been developed for the synthesis of sulfonamides and sulfamates. With the activation by the combination of a catalytic amount of 1-hydroxybenzotriazole (HOBt) and silicon additives, amidations of sulfonyl fluorides and fluorosulfates proceeded smoothly and excellent yields were generally obtained (87-99 %). Noticeably, this protocol is particularly efficient for sterically hindered substrates. Catalyst loading is generally low and only 0.02 mol % of catalyst is required for the multidecagram-scale synthesis of an amantadine derivative. In addition, the potential of this method in medicinal chemistry has been demonstrated by the synthesis of the marketed drug Fedratinib via a key intermediate sulfonyl fluoride 13. Since a large number of amines are commercially available, this route provides a facile entry to access Fedratinib analogues for biological screening.

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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

COA of Formula: C7H13NO2. In 2021 CHEM BIOL DRUG DES published article about FEBRIFUGINE; INHIBITORS; CHEMISTRY; UPDATE in [Prinsloo, Izak F.] North West Univ, Sch Pharm, Pharmaceut Chem, Potchefstroom, South Africa; [Zuma, Nonkululeko H.; Aucamp, Janine; N’Da, David D.] North West Univ, Ctr Excellence Pharmaceut Sci, ZA-2520 Potchefstroom, South Africa in 2021, Cited 32. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7.

Currently available drugs being used to treat leishmaniasis have several shortcomings, including high toxicity, drug administration that requires hospitalization, and the emergence of parasite resistance against clinically used drugs. As a result, there is a dire need for the development of new antileishmanial drugs that are safe, affordable, and efficient. In this study, two new series of synthesized quinazolinone derivatives were investigated as potential future antileishmanial agents, by assessing their activities against theLeishmania(L.)donovaniandL. majorspecies. The cytotoxicity profiles of these derivatives were assessed in vitro on Vero cells. The compounds were found to be safer and without any toxic activities against mammalian cells, compared to the reference drug, halofuginone, a clinical derivative of febrifugine. However, they had demonstrated poor antileishmanial growth inhibition efficacies. The two compounds that had been found the most active were the mono quinazolinone2dand the bisquinazolinone5bwith growth inhibitory efficacies of 35% and 29% for theL. majorandL. donovani9515 promastigotes, respectively. These outcomes had suggested structural redesign,inter aliathe inclusion of polar groups on the quinazolinone ring, to potentially generate novel quinazolinone derivatives, endowed with effective antileishmanial potential.

COA of Formula: C7H13NO2. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Prinsloo, IF; Zuma, NH; Aucamp, J; N’Da, DD or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

I found the field of Chemistry very interesting. Saw the article PIFA-Promoted, Solvent-Controlled Selective Functionalization of C(sp(2))-H or C(sp(3))-H: Nitration via C-N Bond Cleavage of CH3NO2, Cyanation, or Oxygenation in Water published in 2019. Recommanded Product: 177-11-7, Reprint Addresses Kim, MH (corresponding author), Gachon Univ, Coll Pharm, Gachon Inst Pharmaceut Sci, 191 Hambakmoeiro, Incheon 21936, South Korea.. 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 novel nitration (via C(sp(3))-N breaking/C(sp(2))-N formation with CH3NO2) mediated by [bis-(trifluoroacetoxy)iodo]benzene (PIFA) is described. The NO2 transfer from CH3NO2 to the aromatic group of the substrate is possible with careful selection of the solvent, NaX, and oxidant. In addition, the solvent-controlled C(sp(2))-H functionalization can shift to an alpha-C(sp(3))-H functionalization (cyanation or oxygenation) of the alpha-C(sp(3))-H of cyclic amines.

Recommanded Product: 177-11-7. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Mudithanapelli, C; Dhorma, LP; Kim, MH or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

HPLC of Formula: C7H13NO2. 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.

HPLC of Formula: C7H13NO2. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Sahoo, T; Sarkar, S; Ghosh, SC or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem

Yao, ZL; Wang, L; Shao, NQ; Guo, YL; Wang, DH in [Yao, Zhi-Li; Shao, Nan-Qi; Wang, Dong-Hui] Chinese Acad Sci, Shanghai Inst Organ Chem, CAS Key Lab Synthet & Self Assembly Chem Organ Fu, Univ Chinese Acad Sci,Ctr Excellence Mol Synth, 345 Lingling Rd, Shanghai 200032, Peoples R China; [Wang, Lei; Guo, Yin-Long] Chinese Acad Sci, Shanghai Inst Organ Chem, State Key Lab Organometall Chem, Univ Chinese Acad Sci,Ctr Excellence Mol Synth, 345 Lingling Rd, Shanghai 200032, Peoples R China published Copper-Catalyzed ortho-Selective Dearomative C-N Coupling of Simple Phenols with O-Benzoylhydroxylamines in 2019, Cited 82. 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.

A Cu-catalyzed dearomative amination of simple phenols with O-benzoylhydroxylamines (R’RN-OBz) to synthesize alpha-aminocyclohexa-2,4-dienones is reported. This intermolecular transformation occurs exclusively at the position ortho to the hydroxyl group, providing a convenient method to synthesize the desired products in high yields. The reaction proceeds under mild conditions and tolerates a wide range of functional groups. Mechanistic studies indicate that this transformation proceeds via either (1) a single-electron transfer process involving attack of an N-centered radical onto the phenol or (2) a two-electron pathway involving addition of phenol to an electrophilic Cu-III-amino complex via an inner-sphere process.

Recommanded Product: 177-11-7. About 1,4-Dioxa-8-azaspiro[4.5]decane, If you have any questions, you can contact Yao, ZL; Wang, L; Shao, NQ; Guo, YL; Wang, DH or concate me.

Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem