Heterocyclic Building Blocks-piperidine

Kalliokoski, Tuomo; Rummakko, Petteri; Rantanen, Marja; Blaesse, Michael; Augustin, Martin; Ummenthala, Goverdhan Reddy; Choudhary, Sapan; Venalainen, Jarkko published the artcile< Discovery of sulfonamides and 9-oxo-2,8-diazaspiro[5,5]undecane-2-carboxamides as human kynurenine aminotransferase 2 (KAT2) inhibitors>, Application In Synthesis of 91419-53-3, the main research area is human kynurenine aminotransferase 2 KAT2 reversible inhibitor virtual screening; Human kynurenine aminotransferase 2; KAT2; Reversible inhibitor; Virtual screening.

Human kynurenine aminotransferase 2 (KAT2) inhibitors could be potentially used to treat the cognitive deficits associated with bipolar disease and schizophrenia. Although, there has been active drug research activity by several industrial and academic groups in developing KAT2 inhibitors over the years, no such compound has proceeded to the clinics. Here, we report two different chem. series of reversible KAT2 inhibitors with sub-micromolar activities. The first series was identified by a high-throughput screening of a diverse random library and the second one by structure-based virtual screening. Two novel crystal structures of KAT2 complexed with different reversible inhibitors were also deposited to the Protein databank which could be useful for future drug discovery efforts.

Bioorganic & Medicinal Chemistry Letters published new progress about Bipolar disorder. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Application In Synthesis of 91419-53-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wagener, Tobias; Lueckemeier, Lukas; Daniliuc, Constantin G.; Glorius, Frank published the artcile< Interrupted pyridine hydrogenation: Asymmetric synthesis of δ-lactams>, COA of Formula: C7H11NO3, the main research area is delta lactam preparation oxazolidinone substituted pyridine interrupted hydrogenation; asymmetric catalysis; heterogeneous catalysis; hydrogenation; lactams; nitrogen heterocycles.

Metal-catalyzed hydrogenation is an effective method to transform readily available arenes into saturated motifs, however, current hydrogenation strategies are limited to the formation of C-H and N-H bonds. The stepwise addition of hydrogen yields reactive unsaturated intermediates that are rapidly reduced. In contrast, the interruption of complete hydrogenation by further functionalization of unsaturated intermediates offers great potential for increasing chem. complexity in a single reaction step. Overcoming the tenet of full reduction in arene hydrogenation has been seldom demonstrated. In this work the authors report the synthesis of sought-after, enantioenriched δ-lactams from oxazolidinone-substituted pyridines and water by an interrupted hydrogenation mechanism.

Angewandte Chemie, International Edition published new progress about Hydrogenation. 25504-47-6 belongs to class piperidines, and the molecular formula is C7H11NO3, COA of Formula: C7H11NO3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liu, Richard Y.; Bae, Minwoo; Buchwald, Stephen L. published the artcile< Mechanistic Insight Facilitates Discovery of a Mild and Efficient Copper-Catalyzed Dehydration of Primary Amides to Nitriles Using Hydrosilanes>, Name: tert-Butyl 3-cyanopiperidine-1-carboxylate, the main research area is copper catalyst dehydration primary amide hydrosilane; nitrile preparation.

Metal-catalyzed silylative dehydration of primary amides is an economical approach to the synthesis of nitriles. A copper-hydride(CuH)-catalyzed process is reported that avoids a typically challenging 1,2-siloxane elimination step, thereby dramatically increasing the rate of the overall transformation relative to alternative metal-catalyzed systems. This new reaction proceeds at ambient temperature, tolerates a variety of metal-, acid-, or base-sensitive functional groups and can be performed using a simple ligand, inexpensive siloxanes and low catalyst loading.

Journal of the American Chemical Societypublished new progress about Amides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Name: tert-Butyl 3-cyanopiperidine-1-carboxylate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Nakajima, Noriyuki; Ubukata, Makoto published the artcile< Preparation of nitriles from primary amides under Swern oxidation conditions>, Synthetic Route of 91419-53-3, the main research area is Swern oxidation carboxamide; nitrile preparation.

In order to establish a mild conversion method of primary amides to nitriles, various types of carboxamides were treated under Swern oxidation conditions, (COCl)2-DMSO and Et3N, as a dehydrating agent to obtain desired nitriles in 75-96% yields.

Tetrahedron Letterspublished new progress about Amides Role: RCT (Reactant), RACT (Reactant or Reagent). 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Synthetic Route of 91419-53-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wagener, Tobias; Lueckemeier, Lukas; Daniliuc, Constantin G.; Glorius, Frank published the artcile< Interrupted pyridine hydrogenation: Asymmetric synthesis of δ-lactams>, SDS of cas: 25504-47-6, the main research area is delta lactam preparation oxazolidinone substituted pyridine interrupted hydrogenation; asymmetric catalysis; heterogeneous catalysis; hydrogenation; lactams; nitrogen heterocycles.

Metal-catalyzed hydrogenation is an effective method to transform readily available arenes into saturated motifs, however, current hydrogenation strategies are limited to the formation of C-H and N-H bonds. The stepwise addition of hydrogen yields reactive unsaturated intermediates that are rapidly reduced. In contrast, the interruption of complete hydrogenation by further functionalization of unsaturated intermediates offers great potential for increasing chem. complexity in a single reaction step. Overcoming the tenet of full reduction in arene hydrogenation has been seldom demonstrated. In this work the authors report the synthesis of sought-after, enantioenriched δ-lactams from oxazolidinone-substituted pyridines and water by an interrupted hydrogenation mechanism.

Angewandte Chemie, International Editionpublished new progress about Hydrogenation. 25504-47-6 belongs to class piperidines, and the molecular formula is C7H11NO3, SDS of cas: 25504-47-6.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Gross, Kathleen M. Bertini; Beak, Peter published the artcile< Complex-Induced Proximity Effects: The Effect of Varying Directing-Group Orientation on Carbamate-Directed Lithiation Reactions>, SDS of cas: 149518-50-3, the main research area is proximity effect complex induced; carbamate directed lithiation.

A series of selected bicyclic carbamates in which the range of accessible angles and distances between the carbonyl group and the proton removed in an α-lithiation reaction are structurally defined have been investigated. Oxazolidinones I (n = 1, 2; R = i-Pr, t-Bu) undergo stereoselective lithiation-substitution reactions to provide cis-II as the major diastereomers. Two series of competition experiments show that the conformationally restricted carbamates undergo lithiation via complexes more efficiently than Boc amines (e.g., N-Boc-pyrrolidine, N-Boc-piperidine). These results along with semiempirical calculations suggest that a small dihedral angle and a calculated distance of 2.78 Å between the carbamate carbonyl oxygen and the proton to be removed are favorable for a carbamate-directed lithiation. A series of tin-lithium exchange experiments indicate that the configurational stability of a carbamate-stabilized organolithium species may be enhanced by restrictive geometry.

Journal of the American Chemical Societypublished new progress about Chelation (and configurational stability of carbanion intermediate). 149518-50-3 belongs to class piperidines, and the molecular formula is C12H21NO4, SDS of cas: 149518-50-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Amani, Javad; Molander, Gary A. published the artcile< Direct Conversion of Carboxylic Acids to Alkyl Ketones>, Quality Control of 180181-05-9, the main research area is ketone preparation photoredox synergistic catalytic coupling carboxylic acid alkyltrifluoroborate; synergistic photoredox nickel catalytic coupling carboxylic acid alkyltrifluoroborate.

An efficient and mild method for acyl-Csp3 bond formation based on the direct conversion of carboxylic acids has been established. This protocol is enabled by the synergistic, Ir-photoredox/nickel catalytic cross-coupling of in situ activated carboxylic acids and alkyltrifluoroborates. This versatile method is amenable to the cross-coupling of structurally diverse carboxylic acids with various potassium alkyltrifluoroborates, affording the corresponding ketones with high yields. In this operationally simple cross-coupling protocol, aliphatic ketones are obtained in one step from bench stable, readily available carboxylic acids.

Organic Letterspublished new progress about Carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent) (activated). 180181-05-9 belongs to class piperidines, and the molecular formula is C22H23NO4, Quality Control of 180181-05-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Badir, Shorouk O.; Lipp, Alexander; Krumb, Matthias; Cabrera-Afonso, Maria Jesus; Kammer, Lisa Marie; Wu, Victoria E.; Huang, Minxue; Csakai, Adam; Marcaurelle, Lisa A.; Molander, Gary A. published the artcile< Photoredox-mediated hydroalkylation and hydroarylation of functionalized olefins for DNA-encoded library synthesis>, Synthetic Route of 180181-05-9, the main research area is phthalimide ester DNA conjugated trifluoromethyl alkene photoredox catalyst trifluoromethylation; DNA encoded trifluoromethylalkyl aryl amide preparation; alkene DNA conjugated aryl iodide photoredox catalyst reductive alkylation; alkylaryl DNA encoded amide preparation.

DNA-encoded library (DEL) technol. features a time- and cost-effective interrogation format for the discovery of therapeutic candidates in the pharmaceutical industry. To develop DEL platforms, the implementation of water-compatible transformations that facilitate the incorporation of multifunctional building blocks (BBs) with high C(sp3) carbon counts is integral for success. In this report, a decarboxylative-based hydroalkylation of DNA-conjugated trifluoromethyl-substituted alkenes enabled by single-electron transfer (SET) and subsequent hydrogen atom termination through electron donor-acceptor (EDA) complex activation was detailed. In a further photoredox-catalyzed hydroarylation protocol, the coupling of functionalized, electronically unbiased olefins was achieved under air and within minutes of blue light irradiation through the intermediacy of reactive (hetero)aryl radical species with full retention of the DNA tag integrity. Notably, these processes operate under mild reaction conditions, furnishing complex structural scaffolds with a high d. of pendant functional groups.

Chemical Sciencepublished new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 180181-05-9 belongs to class piperidines, and the molecular formula is C22H23NO4, Synthetic Route of 180181-05-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine the name comes from the genus name Piper, which is the Latin word for pepper. 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Related Products of 2403-88-5.

Zuo, Shiyu;Li, Dongya;Guan, Zeyu;Zhu, Yi;Pu, Mengjie;Xia, Dongsheng research published 《 Rapid electron transfer boosts CuO-Mediated nonradical oxidation pathways for efficient removal of Bisphenol A》, the research content is summarized as follows. CO₂ emission reduction and CO₂ capture during wastewater treatment are the main objectives of carbon neutral wastewater treatment. Here, we show that CuO is expected to promote non-radical oxidation pathways through enhanced electron transfer. Calcination temperature may affect crystal growth and microscopic strain, and the smaller particle size of CuO provides shorter distance nanochannels for core-shell diffusion of electrons/defects. This facilitates fast electron transfer and easy in/out diffusion of electrons/defects, thus promotes ¹O₂-mediated nonradical oxidation (13.6-fold increase in kinetic reaction rate). A kinetic model was developed to predict the kinetic reaction rate constants of CuO/peroxymonosulfate (PMS) under different parameter conditions. The degradation pathways and product toxicity of pollutants are explored through Frontier MO Theory (FMO) and the Toxicity Estimation Software Tool (TEST). Due to the alk. environment and the mild oxidation capacity of ¹O₂-mediated nonradical oxidation pathway, CuO/PMS system can not only effectively detoxify toxic organic pollutants without complete mineralization (emitting large amounts of CO₂), but also capture CO₂ and convert it into stable carbonates for environmental use. This study demonstrates the ability of CuO/PMS to effectively treat toxic organic pollutants in a practical microreactor, and provides a viable pathway for carbon neutral wastewater treatment.

2403-88-5, 2,2,6,6-Tetramethyl-4-piperidinol(TEMPO) is a useful research compound. Its molecular formula is C9H19NO and its molecular weight is 157.25 g/mol. The purity is usually 95%.
TEMPO is an intermediate used in the preparation of Piperidinyloxy free radical derivatives.
TEMPO is an organic compound that acts as a radical scavenger. It is stable in the presence of water and air and can be used for the inhibition of bacterial growth. TEMPO reacts with reactive intermediates to form non-reactive substances and terminate chain reactions. This process is optimal at temperatures between 0°C and 40°C and pH values between 3.5 and 7.5. TEMPO has been shown to inhibit the growth of bacteria by reacting with reactive molecules such as amines, chlorides, or low energy radicals in aqueous solution. TEMPO also has genotoxic activity that inhibits DNA synthesis in bacterial cells through oxidation of guanine residues on DNA molecules., Related Products of 2403-88-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). 2403-88-5, formula is C9H19NO, Name is 2,2,6,6-Tetramethyl-4-piperidinol. It is a colorless liquid with an odor described as objectionable, and typical of amines. Recommanded Product: 2,2,6,6-Tetramethyl-4-piperidinol.

Zou, Lijun;Zhu, Xiaoying;Lu, Lun;Xu, Yiliang;Chen, Baoliang research published 《 Bimetal organic framework/graphene oxide derived magnetic porous composite catalyst for peroxymonosulfate activation in fast organic pollutant degradation》, the research content is summarized as follows. A magnetic nitrogen-doped porous carbon material (Co/CoOx@NC) with large surface area was synthesized for peroxymonosulfate (PMS) activation. The addition of reduced graphene oxide (rGO) remarkably improved the catalytic performance of Co/CoOx@NC due to its enhancement on graphitization degree and structural regulation. Co/CoOx@NC exhibited excellent PMS activation for phenol removal with almost 100% removal efficiency in 10 min, close to that of homogeneous Co²⁺. Simultaneously, good reusability and recyclability of Co/CoOx@NC was achieved, demonstrating its feasibility for practical application. The PMS activation process in Co/CoOx@NC/PMS system was dominant by efficient mediation of electron transfer from pollutants to PMS through the sp2-hybridized carbon and nitrogen network. Batch tests of various organic compounds removal revealed the specific selectivity related to the electron-donating ability in Co/CoOx@NC/PMS system. As the negligible role of reactive radicals on pollutants degradation, the inhibition of interfering species (e.g., Cl^–, natural organic matters) was largely weakened. Present study not only provided a strategy for rationally designing highly efficient nanocarbon-based catalysts on PMS activation, but also presented new insight into the mechanism of PMS heterogeneous activation.

Recommanded Product: 2,2,6,6-Tetramethyl-4-piperidinol, 2,2,6,6-Tetramethyl-4-piperidinol(TEMPO) is a useful research compound. Its molecular formula is C9H19NO and its molecular weight is 157.25 g/mol. The purity is usually 95%.
TEMPO is an intermediate used in the preparation of Piperidinyloxy free radical derivatives.
TEMPO is an organic compound that acts as a radical scavenger. It is stable in the presence of water and air and can be used for the inhibition of bacterial growth. TEMPO reacts with reactive intermediates to form non-reactive substances and terminate chain reactions. This process is optimal at temperatures between 0°C and 40°C and pH values between 3.5 and 7.5. TEMPO has been shown to inhibit the growth of bacteria by reacting with reactive molecules such as amines, chlorides, or low energy radicals in aqueous solution. TEMPO also has genotoxic activity that inhibits DNA synthesis in bacterial cells through oxidation of guanine residues on DNA molecules., 2403-88-5.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem