22-Sep-2021 News Can You Really Do Chemisty Experiments About 177-11-7

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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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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7618N – PubChem

 

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Thirty novel 9-fluoro-2,3-dihydro-8,10-(mono/di-sub)-3-methyl-8-nitro-7-oxo-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acids were synthesized from 2,3,4,5-tetrafluoro benzoic acid and evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis H37Rv (MTB), multi-drug resistant Mycobacterium tuberculosis (MDR-TB), and Mycobacterium smegmatis (MC2) and also tested for the ability to inhibit the supercoiling activity of DNA gyrase from mycobacteria. Among the synthesized compounds, 10-[2-carboxy-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-9-fluoro-2,3-dihydro-3-methyl-8-nitro-7-oxo-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid was found to be the most active compound in vitro with MIC99 of 0.19 muM and 0.09 muM against MTB and MTR-TB, respectively. In the in vivo animal model also the same compound decreased the bacterial load in lung and spleen tissues with 1.91 and 2.91 – log 10 protections, respectively, at the dose of 50 mg/kg body weight. Compound 10-[(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)]-9-fluoro-2,3-dihydro-3-methyl-8-nitro-7-oxo-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid was found to be the most active in the inhibition of the supercoiling activity of DNA gyrase with an IC50 of 10.0 mug/mL. The results demonstrate the potential and importance of developing new oxazino quinolone derivatives against mycobacterial infections.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7207N – PubChem

 

18-Sep-2021 News Properties and Exciting Facts About 177-11-7

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The present invention relates to processes for synthesizing piperazine-piperidine compounds, and compounds useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. The processes also allow for safer and environmentally tolerant production of these useful compounds.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7261N – PubChem

 

17/9/2021 News Final Thoughts on Chemistry for 177-11-7

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent, Application In Synthesis of 1,4-Dioxa-8-azaspiro[4.5]decane, Which mentioned a new discovery about 177-11-7

Unprotected secondary amines are directly alkylated by C-H functionalization adjacent to nitrogen, thereby opening new routes toward the synthesis of alpha- and beta-alkylated N-heterocycles. alpha-Alkylated piperidine, piperazine, and azepane products are prepared from heterocycles and alkenes in an atom-economic reaction with excellent regio- and diastereoselectivity. beta-Alkylated N-heterocycles are synthesized via a scalable one-pot alkylation/cyclization procedure generating 3-methylated azetidines, pyrrolidines, and piperidines.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7176N – PubChem

 

16-Sep News Properties and Exciting Facts About 177-11-7

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A one-pot, isocyanide based multicomponent protocol was presented starting from secondary amines towards (thio)urea derivatives and utilized for the construction of a diverse 27-membered chemical library. Following a green compatible microwave assisted condition, the formed N,N?-multisubstituted (thio)ureas were obtained in up to 85% yield.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7749N – PubChem

 

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A formal anti-Markovnikov hydroamination of allylic alcohols using a Ru catalyst via tandem oxidation/1,4-conjugate addition/1,2-reduction was developed. Thus, the reaction of allylic alcohols with amines was performed in the presence of the catalyst generated from RuClH(CO)(PPh3)3 and 2,6-bis(n-butyliminomethyl)pyridine in situ to afford the corresponding gamma-amino alcohols efficiently. This journal is

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7782N – PubChem

 

15/9/2021 News A new application about 177-11-7

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Simultaneous inhibition of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) has recently been validated as a potentially novel therapeutic approach for Alzheimer’s disease (AD). To further extend this concept, we designed and synthesized the first chemical series of dual acting PDE5 and HDAC inhibitors, and we validated this systems therapeutics approach. Following the implementation of structure- and knowledge-based approaches, initial hits were designed and were shown to validate our hypothesis of dual in vitro inhibition. Then, an optimization strategy was pursued to obtain a proper tool compound for in vivo testing in AD models. Initial hits were translated into molecules with adequate cellular functional responses (histone acetylation and cAMP/cGMP response element-binding (CREB) phosphorylation in the nanomolar range), an acceptable therapeutic window (>1 log unit), and the ability to cross the blood-brain barrier, leading to the identification of 7 as a candidate for in vivo proof-of-concept testing (Cuadrado-Tejedor, M.; Garcia-Barroso, C.; Sanchez-Arias, J. A.; Rabal, O.; Mederos, S.; Ugarte, A.; Franco, R.; Segura, V.; Perea, G.; Oyarzabal, J.; Garcia-Osta, A. Neuropsychopharmacology 2016, in press, doi: 10.1038/npp.2016.163).

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7484N – PubChem

 

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Application In Synthesis of 1,4-Dioxa-8-azaspiro[4.5]decane, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 177-11-7, Name is 1,4-Dioxa-8-azaspiro[4.5]decane, molecular formula is C7H13NO2. In a Article, authors is Lemiegre, Loic,once mentioned of 177-11-7

Treatment of [60] or [70]fullerene with excess secondary amine and 3 equiv. of cumene hydroperoxide regioselectively afforded a mono-oxygenated tetraamino or diamino fullerene in good to high yield. The reaction is operationally simple and applicable to a large-scale synthesis. Copyright

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7180N – PubChem

 

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Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro and in vivo potency and acceptable physical properties.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7174N – PubChem

 

Sep 2021 News More research is needed about 177-11-7

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Chemistry is traditionally divided into organic and inorganic chemistry. Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent,Which mentioned a new discovery about 177-11-7

The disclosure provides compounds of Formula I, which may be useful as aldehyde dehydrogenase inhibitors and the pharmaceutically acceptable salts thereof. The variables, J, R4, G, Q, and ring A are defined herein. Aldehyde dehydrogenase inhibitors of Formula I are useful for treating a variety of conditions including cancer and inflammation. The disclosure includes methods for using compounds and salts of Formula I to treat colon cancer, pancreatic cancer, nasopharyngeal carcinoma, thyroid cancer, prostate cancer, ovarian cancer, head and neck squamous cell carcinoma, lung cancer, hepatocellular carcinoma, leukemia, brain tumorsbreast cancer, atherosclerosis, ischaemic heart disease, acne vulgaris, asthma, autoimmune diseases, autoinflammatory diseases, chronic prostatitis, glomerulonephritis, inflammatory bowel disease, pelvic inflammatory disease, reperfusion injury, rheumatoid arthritis, sarcoidosis, transplant rejection, vasculitis, and interstitial cystitis. The disclosure also includes pharmaceutical compositions containing a compound or salt of Formula I.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H7435N – PubChem