Heterocyclic Building Blocks-piperidine

Crich, David published the artcileCyclofunctionalization of unsaturated alcohols, phenols, acids, and sulfonamides with 1-benzenesulfinyl piperidine and trifluoromethanesulfonic anhydride, HPLC of Formula: 4972-31-0, the publication is Heterocycles (2004), 827-830, database is CAplus.

The combination of a benzenesulfinamide, trifluoromethanesulfonic anhydride, and Huenig’s base brings about the cyclofunctionalization of unsaturated alcs., phenols, acids, and sulfonamides to give the corresponding α-phenylsulfanylmethyl cyclic ethers, lactones and sulfonamides, resp. In an unanticipated twist the products are isolated at the sulfur (II) oxidation state denoting an overall reduction in the oxidation state of the sulfur based electrophile in the course of the reaction.

Heterocycles 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 C11H15NOS, HPLC of Formula: 4972-31-0.

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

Jose, Gilish published the artcileSynthesis, molecular docking, antimycobacterial and antimicrobial evaluation of new pyrrolo[3,2-c]pyridine Mannich bases, HPLC of Formula: 39546-32-2, the publication is European Journal of Medicinal Chemistry (2017), 275-288, database is CAplus and MEDLINE.

In this report, we describe the synthesis and biol. evaluation of a new series of pyrrolo[3,2-c]pyridine Mannich bases. The Mannich bases were obtained in good yields by one-pot three component condensation of pyrrolo[3,2-c]pyridine scaffold with secondary amines and excess of formaldehyde solution in AcOH. The chem. structures of the compounds were characterized by ¹H NMR, ¹³C NMR, LC/MS and elemental anal. Single crystal X-ray diffraction has been recorded for compound I ([C₂₃H₂₉ClN₄]⁺², H₂O). The in vitro antimicrobial activities of the compounds were evaluated against various bacterial and fungal strains using Agar diffusion method and Broth micro dilution method. Compounds II (n = 1, R = 4-Me-piperazin-1-yl, N-Bn-ethanamino; n = 2, R = N-Me-2-Ph-ethanamine, piperidine-3-carboxamide, piperidine-4-carboxamide) were showed good Gram-pos. antibacterial activity against S. aureus, B. flexus, C. sporogenes and S. mutans. Furthermore, in vitro antimycobacterial activity was evaluated against Mycobacterium tuberculosis H37Rv (ATCC 27294) using MABA. Compounds II (n = 2, R = N-Me-2-Ph-ethanamine, piperidine-3-carboxamide, piperidine-4-carboxamide) were showed good antitubercular activity against Mtb (MIC ≥6.25 μg/mL). Among the tested compounds, II (n = 2, R = piperidine-3-carboxamide) was showed excellent antimycobacterial activity against Mtb (MIC <0.78 μg/mL) and low cytotoxicity against the HEK-293T cell line (SI >>25). Mol. docking of the active compounds against glutamate racemase (MurI) and Mtb glutamine synthetase were explained the structure-activity observed in vitro.

European Journal of 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, HPLC of Formula: 39546-32-2.

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

Jose, Gilish published the artcileNew polyfunctional imidazo[4,5-C]pyridine motifs: Synthesis, crystal studies, docking studies and antimicrobial evaluation, Related Products of piperidines, the publication is European Journal of Medicinal Chemistry (2014), 288-297, database is CAplus and MEDLINE.

New antimicrobial agents, imidazo[4,5-c]pyridine derivatives were synthesized. The authors have developed a new synthetic protocol for the final reaction, an efficient microwave-assisted synthesis of imidazo[4,5-c]pyridines from substituted 3,4-diaminopyridine and carboxylic acids in presence of DBU mediated by T3P. The chem. structures of the new compounds were characterized by IR, ¹H NMR, ¹³C NMR, mass spectral anal. and elemental anal. In addition, single crystal x-ray diffraction also was recorded for compound 1-(7-(3-Fluorophenyl)-2-(phenoxymethyl)-1H-imidazo[4,5c]pyridin-4-yl)piperidine-3-carbonitrile. The in vitro antimicrobial activities of the compounds were conducted against various Gram-neg., Gram-pos. bacteria and fungi. Amongst the tested, seven compounds displayed promising antimicrobial activity. The mol. docking of GlcN-6-P synthase with newly synthesized compounds was carried out.

European Journal of 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, Related Products of piperidines.

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

Wei, Juhong published the artciletert-Butyl Sulfoxide as a Starting Point for the Synthesis of Sulfinyl Containing Compounds, COA of Formula: C11H15NOS, the publication is Organic Letters (2015), 17(21), 5396-5399, database is CAplus and MEDLINE.

Sulfoxides bearing a tert-Bu group can be activated using N-bromosuccinimide (NBS) under acidic conditions and then subsequently treated with a variety of nitrogen, carbon, or oxygen nucleophiles to afford a wide range of the corresponding sulfinic acid amides, new sulfoxides, and sulfinic acid esters.

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 C9H5ClO2, COA of Formula: C11H15NOS.

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

Wu, Xuan published the artcileActivation of peroxymonosulfate by magnetic CuFe₂O₄@ZIF-67 composite catalyst for the study on the degradation of methylene blue, Name: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Colloids and Surfaces, A: Physicochemical and Engineering Aspects (2022), 128278, database is CAplus.

In this research, a novel magnetically recoverable composite catalyst, CuFe₂O₄ @ZIF-67, was synthesized. CuFe₂O₄@ZIF-67 composite catalyst was applied to degrade methylene blue (MB) in water by activating peroxymonosulfate (PMS). The results showed that the degradation rate of MB (20 mg/L) reached 98.9% in 30 min in the 0.2-CuFe₂O₄@ZIF-67 (75 mg/L) + PMS (125 mg/L) system. Both ESR (EPR) studies and radical quenching experiments revealed that SO^–₄•, •OH, ¹O₂ and •O^–₂ were involved in the degradation of MB. We proposed a catalytic mechanism of PMS activation by CuFe₂O₄@ZIF-67. With the synergistic effect of Co³⁺/Co²⁺, Fe³⁺/Fe²⁺ and Cu²⁺/Cu⁺ redox cycles, it can keep its outstanding catalytic activity. Recycling tests showed that the removal rate of MB can still be maintained above 85%, indicating that CuFe₂O₄@ZIF-67 has good reusability. In general, owing to its reusability and excellent catalytic activity, the CuFe₂O₄@ZIF-67 composite catalyst has a good application prospect in water pollution control.

Colloids and Surfaces, A: Physicochemical and Engineering Aspects 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 C4H6BrFO2, Name: 2,2,6,6-Tetramethylpiperidin-4-one.

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

Cueto-Diaz, Eduardo J. published the artcileCO₂ adsorption capacities of amine-functionalized microporous silica nanoparticles, Formula: C19H21N, the publication is Reactive & Functional Polymers (2022), 105100, database is CAplus.

Efforts on CO₂ capture have intensified as climate change compromises ecosystems and biodiversity. Therefore, it is crucial to develop different methods for CO₂ sequestration to improve solid sorbent capabilities (NPs). To this end, the surface of 200-nm silica nanoparticles (SiO₂NPs) was covalently anchored with aminated ligands, 3-aminopropyltriethoxysilane (APTES), poly(amidoamine) dendrimers (PAMAM) and a short peptide comprising two lysine units, aiming for CO₂ adsorption over a wide range of pressures. Our goal was to explore the influence of functional chem. groups (attached to the SiO₂NPs) on CO₂ sequestration. The observed results showed that at low and high CO₂ gas pressure conditions, typical APTES functionalized SiO₂Np surpassed the CO₂ adsorption capacities of dendritic and peptide-based nanoparticles bearing amine-polymer functionalities, a remarkable effect that was investigated in this work. In addition, a convenient and facile method to decorate and quantify SiO₂ nanoparticles with PAMAM and a short peptide is reported.

Reactive & Functional Polymers 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, Formula: C19H21N.

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

Gerleve, Carolin published the artcileTransition-Metal-Free Oxidative Cross-Coupling of Tetraarylborates to Biaryls Using Organic Oxidants, Quality Control of 219543-09-6, the publication is Angewandte Chemie, International Edition (2020), 59(36), 15468-15473, database is CAplus and MEDLINE.

Readily prepared tetraarylborates undergo selective (cross)-coupling through oxidation with Bobbitt’s salt to give sym. and unsym. biaryls. The organic oxoammonium salt can be used either as a stoichiometric oxidant or as a catalyst in combination with in situ generated NO₂ and mol. oxygen as the terminal oxidant. For selected cases, oxidative coupling is also possible with NO₂/O₂ without any addnl. nitroxide-based cocatalyst. Transition-metal-free catalytic oxidative ligand cross-coupling of tetraarylborates is unprecedented and the introduced method provides access to various biaryl and heterobiaryl systems.

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 C11H21BF4N2O2, Quality Control of 219543-09-6.

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

Iniguez, Amanda Balboni published the artcileEWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma, Category: piperidines, the publication is Cancer Cell (2018), 33(2), 202-216.e6, database is CAplus and MEDLINE.

Many cancer types are driven by oncogenic transcription factors that have been difficult to drug. Transcriptional inhibitors, however, may offer inroads into targeting these cancers. Through chem. genomics screening, we identified that Ewing sarcoma is a disease with preferential sensitivity to THZ1, a covalent small-mol. CDK7/12/13 inhibitor. The selective CDK12/13 inhibitor, THZ531, impairs DNA damage repair in an EWS/FLI-dependent manner, supporting a synthetic lethal relationship between response to THZ1/THZ531 and EWS/FLI expression. The combination of these mols. with PARP inhibitors showed striking synergy in cell viability and DNA damage assays in vitro and in multiple models of Ewing sarcoma, including a PDX, in vivo without hematopoietic toxicity.

Cancer Cell published new progress about 1702809-17-3. 1702809-17-3 belongs to piperidines, auxiliary class Cell Cycle,CDK, name is (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide, and the molecular formula is C30H32ClN7O2, Category: piperidines.

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

Lambert, Kyle M. published the artcileEnhancement of the Oxidizing Power of an Oxoammonium Salt by Electronic Modification of a Distal Group, Name: 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, the publication is Journal of Organic Chemistry (2017), 82(21), 11440-11446, database is CAplus and MEDLINE.

The multigram preparation and characterization of a novel TEMPO-based oxoammonium salt, 2,2,6,6-tetramethyl-4-(2,2,2-trifluoroacetamido)-1-oxopiperidinium tetrafluoroborate (5), and its corresponding nitroxide (4) are reported. The solubility profile of 5 in solvents commonly used for alc. oxidations differs substantially from that of Bobbitt’s salt, 4-acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium tetrafluoroborate (1). The rates of oxidation of a representative series of primary, secondary, and benzylic alcs. by 1 and 5 in acetonitrile solvent at room temperature have been determined, and oxoammonium salt 5 has been found to oxidize alcs. more rapidly than does 1. The rate of oxidation of meta- and para-substituted benzylic alcs. by either 1 or 5 displays a strong linear correlation to Hammett parameters (r > 0.99) with slopes (ρ) of -2.7 and -2.8, resp., indicating that the rate-limiting step in the oxidations involves hydride abstraction from the carbinol carbon of the alc. substrate.

Journal of Organic Chemistry 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, Name: 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate.

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

Entooru, Keshamma published the artcileGC-MS analysis of bioactive components and evaluation of in-vitro pancreatic lipase inhibitory activity of aqueous extracts of Pleurotus eryngii, Application In Synthesis of 826-36-8, the publication is International Journal of Chemical Studies (2021), 9(2), 1141-1145, database is CAplus.

Present study was designed to conduct with main purpose to determine bioactive components and evaluation of aqueous extract of Pleurotus eryngii for in-vitro pancreatic lipase inhibitory activity. GC-MS anal. was carried out to determine the bioactive components and in-vitro pancreatic lipase inhibitory assay was carried out to determine IC50 values of aqueous extracts of Pleurotus eryngii. The results of the present study depicted that the aqueous extracts of Pleurotus eryngii possess in-vitro pancreatic lipase inhibitory activities at the concentration of 1-30μg/mL and this could be attributed to the prevailing compounds identified in the GC-MS anal. i.e., conhydrin, di-Et phthalate, phthalic acid-Bu hex-3-yl ester (alkaloids), ar-turmerone (sesquiterpenoid), palmitic acid, myristic acid, phenol and benzoic acid from ethanolic extract of Pleurotus eryngii. In conclusion, polyphenols, alkaloids terpenoids and Vitamin B class of secondary metabolites majorly identified in GC-MS anal. of aqueous extract of Pleurotus eryngii has been reported to possess the in-vitro pancreatic lipase inhibitory activities. Hence, further in-vivo studies in exptl. induced obese animal models could be recommended to access the safety and efficacy of aqueous extracts of Pleurotus eryngii to strongly recommend them as natural antiobesity agents in the formulations of natural antiobesity drugs.

International Journal of Chemical Studies 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, Application In Synthesis of 826-36-8.

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