Day: November 30, 2022

Wimmer, Alexander published the artcileN-Arylation of NH-Sulfoximines via Dual Nickel Photocatalysis, HPLC of Formula: 4972-31-0, the publication is Organic Letters (2019), 21(8), 2740-2744, database is CAplus and MEDLINE.

The pharmaceutically underexplored sulfoximine moiety has emerged as a potentially active pharmaceutical ingredient. We developed a scalable synthetic route to N-arylated sulfoximines from the resp. “free” NH-sulfoximines and bromoarenes. Our strategy is based on a dual nickel photocatalytic approach, is applicable for a broad scope of substrates, and exhibits a highly functional group tolerance. In addition, we could demonstrate that other sulfoximidoyl derivatives like sulfonimidamides and sulfinamides proceed smoothly under the developed reaction conditions.

Organic Letters published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C15H16O3, HPLC of Formula: 4972-31-0.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Wertz, Sebastian published the artcileAmination of Benzoxazoles and 1,3,4-Oxadiazoles Using 2,2,6,6-Tetramethylpiperidine-N-oxoammonium Tetrafluoroborate as an Organic Oxidant, Category: piperidines, the publication is Angewandte Chemie, International Edition (2011), 50(48), 11511-11515, S11511/1-S11511/116, database is CAplus and MEDLINE.

No transition metals are necessary to convert benzoxazoles and 1,3,4-oxadiazoles into the corresponding pharmacol. interesting 2-aminated heterocycles by formal direct C(2)-amination using tetramethylpiperidine-N-oxoammonium tetrafluoroborate (TEMPO⁺BF₄^–) as an oxidant. Mechanistic studies were carried out, and the methodol. was also applied to the preparation of racemic MK-4305.

Angewandte Chemie, International Edition published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C3H5BN2O2, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Kuroda, Shoichi published the artcileSynthesis and structure-activity relationship of C-phenyl D-glucitol (TP0454614) derivatives as selective sodium-dependent glucose cotransporter 1 (SGLT1) inhibitors, Recommanded Product: Piperidine-4-carboxamide, the publication is Chemical & Pharmaceutical Bulletin (2020), 68(7), 635-652, database is CAplus and MEDLINE.

Sodium-glucose cotransporter 1 (SGLT1) is the primary transporter for glucose absorption from the gastrointestinal tract. While C-Ph d-glucitol derivative SGL5213 has been reported to be a potent intestinal SGLT1 inhibitor for use in the treatment of type 2 diabetes, no SGLT1 selectivity was found in vitro (IC50 29 nM for hSGLT1 and 20 nM for hSGLT2). In this study we found a new method of synthesizing key intermediates 12 by a one-pot three-component condensation reaction and discovered C-Ph d-glucitol 41j (TP0454614), which has >40-fold SGLT1 selectivity in vitro (IC₅₀ 26 nM for hSGLT1 and 1101 nM for hSGLT2). The results of our study have provided new insights into the structure-activity relationships (SARs) of the SGLT1 selectivity of C-glucitol derivatives

Chemical & Pharmaceutical Bulletin published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Recommanded Product: Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Kosak, Urban published the artcileN-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer’s agents, Name: Piperidine-4-carboxamide, the publication is Bioorganic & Medicinal Chemistry (2017), 25(2), 633-645, database is CAplus and MEDLINE.

In the brains of patients with Alzheimer’s disease, the enzymic activities of butyrylcholinesterase (BChE) and monoamine oxidase B (MAO-B) are increased. While BChE is a viable therapeutic target for alleviation of symptoms caused by cholinergic hypofunction, MAO-B is a potential therapeutic target for prevention of neurodegeneration in Alzheimer’s disease. Starting with piperidine-based selective human (h)BChE inhibitors and propargylamine-based MAO inhibitors, the authors have designed, synthesized and biochem. evaluated a series of N-propargylpiperidines. All of these compounds inhibited hBChE with good selectivity over the related enzyme, acetylcholinesterase, and crossed the blood-brain barrier in a parallel artificial membrane permeation assay. The crystal structure of one of the inhibitors (compound 3) in complex with hBChE revealed its binding mode. Three compounds (4, 5, and 6) showed concomitant inhibition of MAO-B. Addnl., the most potent hBChE inhibitor 7 and dual BChE and MAO-B inhibitor 6 were non-cytotoxic and protected neuronal SH-SY5Y cells from toxic amyloid β-peptide species.

Bioorganic & Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Name: Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Eissler, Stefan published the artcileSubstitution determination of Fmoc-substituted resins at different wavelengths, Computed Properties of 35661-58-6, the publication is Journal of Peptide Science (2017), 23(10), 757-762, database is CAplus and MEDLINE.

In solid-phase peptide synthesis, the nominal batch size is calculated using the starting resin substitution and the mass of the starting resin. The starting resin substitution constitutes the basis for the calculation of a whole set of important process parameters, such as the number of amino acid derivative equivalent For Fmoc-substituted (Fmoc = 9-fluorenyl-methoxycarbonyl) resins, substitution determination is often performed by suspending the Fmoc-protected starting resin in 20% (volume/volume) piperidine in DMF to generate the dibenzofulvene-piperidine adduct that is quantified by UV-visible spectroscopy. The spectrometric measurement is performed at the maximum absorption wavelength of the dibenzofulvene-piperidine adduct, i.e., at 301.0 nm. The recorded absorption value, the resin weight and the volume are entered into an equation derived from Lambert-Beer’s law, together with the substance-specific molar absorption coefficient at 301.0 nm, in order to calculate the nominal substitution. To our knowledge, molar absorption coefficients between 7100 l mol^-1 cm^-1 and 8100 l mol^-1 cm^-1 have been reported for the dibenzofulvene-piperidine adduct at 301.0 nm. Depending on the applied value, the nominal batch size may differ up to 14%. In this publication, a determination of the molar absorption coefficients at 301.0 and 289.8 nm is reported. Furthermore, proof is given that by measuring the absorption at 289.8 nm the impact of wavelength accuracy is reduced. StartCopText© 2017 The Authors Journal of Peptide Science published by European Peptide Society and John Wiley & Sons Ltd.

Journal of Peptide Science published new progress about 35661-58-6. 35661-58-6 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-((9H-Fluoren-9-yl)methyl)piperidine, and the molecular formula is C19H21N, Computed Properties of 35661-58-6.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Hinkes, Stefan P. A. published the artcileVirtues of Volatility: A Facile Transesterification Approach to Boronic Acids, Recommanded Product: Piperidin-4-ylboronic acid hydrochloride, the publication is Organic Letters (2019), 21(9), 3048-3052, database is CAplus and MEDLINE.

Boronic acids are an increasingly important compound class for many applications, including C-C bond formation reactions, medicinal chem., and diagnostics. The deprotection of boronic ester intermediates is frequently a problematic and inefficient step in boronic acid syntheses. The authors describe an approach that highly facilitates this transformation by leveraging the volatility of methylboronic acid and its diol esters. The method was performed under mild conditions, provides high yields, and eliminates cumbersome and problematic purification steps.

Organic Letters published new progress about 2306405-20-7. 2306405-20-7 belongs to piperidines, auxiliary class Boronic acid and ester,Boronic acid and ester, name is Piperidin-4-ylboronic acid hydrochloride, and the molecular formula is C5H13BClNO2, Recommanded Product: Piperidin-4-ylboronic acid hydrochloride.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Kawale, Harshal D. published the artcileProduction of hydrocarbons from a green algae (Oscillatoria) with exploration of its fuel characteristics over different reaction atmospheres, Safety of 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Energy (Oxford, United Kingdom) (2019), 344-355, database is CAplus.

Authors conducted non-catalytic, catalytic, and hydropyrolysis at 550°C temperature and 1 bar pressure to produce biofuels from an ignored algal biomass of Oscillatoria by thermo-chem. degradation study in a tubular reactor having an internal diameter of 25 mm and 300 mm of active length covered by a furnace of a single heating zone. The catalysts used for the catalytic pyrolysis and hydropyrolysis study are TiO₂:ZnO on 1:1 basis. Characterization of bio-oils by Fourier Transform IR Spectroscopy (FTIR) shows substantial variation in functional groups of all three types of bio-oils. Gas Chromatog.-Mass Spectroscopy (GCMS) gives a detailed list of available hydrocarbons in bio-oil samples and proton NMR confirms the functionality of bio-oil by available proton assignments. Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD) shows morphol. and the structural analogy of biochars with respect to biomass. Calorific values of three types of bio-oils ranges from 16.597 to 16.664 MJ/kg; and revealed that this particular biomass has potential as a resource of feedstock with an approx. yield of one-third of biomass on the dry weight basis. The pH of these bio-oils obtained from green algae varies in the range of 8.25 to 6.07 that indicates the less number of oxygenated compounds unlike very low pH bio-oils obtained from other types of biomass feedstock. Addnl., present results revealed that these bio-oils include formative compounds of most popular hydrocarbons, i.e., benzene, toluene and xylene (BTX). Further, they also include furans, phenols, benzaldehyde, guaiacol, caprolactam, styrene, oximes, etc. which can be used as green chems.

Energy (Oxford, United Kingdom) published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Safety of 2,2,6,6-Tetramethylpiperidin-4-one.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Yamada, Takeshi published the artcileHighly efficient synthesis of oligo-N-acetyl-glucosamines by iterative glycosylation of Di- and tetrachlorophthaloyl-protected thio-glucosamines, Related Products of piperidines, the publication is Chemistry Letters (2005), 34(11), 1556-1557, database is CAplus.

The iterative stereoselective glycosylation of di- and tetrachlorophthaloyl-protected thio-glucosamines, which act as both glycosyl donors and acceptors, gives the corresponding protected oligo-glucosamines. Subsequent removal of the protecting groups followed by acetylation of the free amines affords oligo-N-acetyl-glucosamines in good to excellent combined yields.

Chemistry Letters published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C7H8BBrO3, Related Products of piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Kashparova, V. P. published the artcileThe “one-pot” synthesis of 2,5-diformylfuran, a promising synthon for organic materials in the conversion of biomass, Quality Control of 219543-09-6, the publication is Russian Chemical Bulletin (2015), 64(5), 1069-1073, database is CAplus.

The organic ionic oxidant 4-acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium tetrafluoroborate, [Pip*(O)][BF₄], was found to be compatible with both classical organic solvents and the ionic liquids [BMIm][Cl]/[BMIm][BF₄] (BMIm is 1-butyl-3-methylimidazolium), which are essential in the conversion of cellulose biomass. A unique NMR monitoring procedure developed in our group was used to study the conversion of fructose to 2,5-diformylfuran in ionic liquids This process can successfully be carried out in a “one-pot” fashion; [Pip*(O)][BF₄] efficiently oxidizes intermediate 5-hydroxymethylfurfural. The reaction is highly selective, giving 2,5-diformylfuran in 95% yield.

Russian Chemical Bulletin published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, Quality Control of 219543-09-6.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem