Heterocyclic Building Blocks-piperidine

Yu, Tao; Tagat, Jayaram R.; Kerekes, Angela D.; Doll, Ronald J.; Zhang, Yonglian; Xiao, Yushi; Esposite, Sara; Belanger, David B.; Curran, Patrick J.; Mandal, Amit K.; Siddiqui, M. Arshad; Shih, Neng-Yang; Basso, Andrea D.; Liu, Ming; Gray, Kimberly; Tevar, Seema; Jones, Jennifer; Lee, Suining; Liang, Lianzhu; Ponery, Samad; Smith, Elizabeth B.; Hruza, Alan; Voigt, Johannes; Ramanathan, Lata; Prosise, Winifred; Hu, Mengwei published the artcile< Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core>, Category: piperidines, the main research area is imidazopyrazine pyrazolyl isothiazolylamino derivative preparation aurora kinase inhibition activity; pyrazolyl isothiazolylamino imidazopyrazine solubility antitumor activity; Aurora kinase inhibitors; SCH 1473759; aqueous solubility; cell potency; imidazo-[1,2-a]-pyrazine; tumor xenograft model.

The imidazo-[1,2-a]-pyrazine I is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 μM). Lead optimization guided by the binding mode led to the acyclic amino alc. II (SCH 1473759), which is a picomolar inhibitor of Aurora kinases (TdF Kd Aur A = 0.02 nM and Aur B = 0.03 nM) with improved cell potency (phos-HH3 inhibition IC50 = 25 nM) and intrinsic aqueous solubility (11.4 mM). It also demonstrated efficacy and target engagement in human tumor xenograft mouse models.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Category: piperidines.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chen, Yilin; Du, Jianbo; Zuo, Zhiwei published the artcile< Selective C-C Bond Scission of Ketones via Visible-Light-Mediated Cerium Catalysis>, Application of C7H11NO3, the main research area is hydrazine regioselective preparation photochem; ketone DIAD photochem carbon bond cleavage cerium catalyst.

A general catalytic manifold for selective C-C bond scission of ketones via exploitation of ligand-to-metal charge transfer (LMCT) excitation mode was reported. Through a cooperative utilization of Lewis acid catalysis and LMCT catalysis, the C-C bond of ketones could be selectively and effectively cleaved, enabling installation of different functionalities at each carbon of cleaved C-C bond through a sequential and orthogonal manner. This reaction manifold served as a photocatalytic alternative to Norrish type I reaction with combination of visible light and inexpensive cerium salts. Under operationally simple conditions, a wide range of acyclic and cyclic ketones, from simple strained cyclobutanones to complex androsterone with less strained cyclopentanone moiety, could be successfully transformed into versatile chem. building blocks.

Chem published new progress about Bond cleavage catalysts (C-C, regioselective). 25504-47-6 belongs to class piperidines, and the molecular formula is C7H11NO3, Application of C7H11NO3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Blahun, Oleksandr P.; Melnychenko, Heorhii; Kuchkovska, Yuliya O.; Zhersh, Serhii; Tolmachev, Andrey A.; Grygorenko, Oleksandr O. published the artcile< Synthesis of Functionalized Bridged Bicyclic Sulfonamides with a Bridgehead Nitrogen Atom>, Quality Control of 91419-53-3, the main research area is dioxothiazabicycloalkanecarboxylate bridged sultam preparation.

Sultams with bridgehead nitrogen atoms such as I and II were prepared Dioxothiazabicycloalkanecarboxylic acids such as I with carboxylic acid-substituted bridgehead atoms were prepared in seven steps from Boc-protected azaheterocyclylcarbonitriles such as tert-Bu 3-cyano-1-pyrrolidinecarboxylate by chloromethylation, substitution with a thiolate, oxidative chlorination, substitution of the sulfonyl chloride with fluoride, Boc deprotection, base-mediated cyclization, and nitrile hydrolysis. Dioxothiazabicycloalkanecarboxylic acids such as I with carboxylic acid-substituted bridging atoms were prepared by carboxylation of bridged sultams [prepared in six steps by literature procedures from Boc-protected (hydroxymethyl)azacycles]. Two approaches to the synthesis of functionalized bridged bicyclic sulfonamides with a bridgehead nitrogen atom were developed. Both types of bridged sultams were prepared on > 1g scales.

European Journal of Organic Chemistry published new progress about Carboxylation. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Quality Control of 91419-53-3.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zacharie, Boulos; Abbott, Shaun D.; Baigent, Christopher B.; Doyle, Christopher; Yalagala, Ravi Shekar published the artcile< An Efficient Two-Step Preparation of α-, β-, γ- or δ-Amino Acids from 2-Pyrazinones, 2-Hydroxypyrimidines or 2-Pyridones Respectively>, Electric Literature of 25504-47-6, the main research area is amino acid alpha beta gamma preparation pyrazinone hydroxypyrimidine pyridone.

A practical and efficient two-step procedure is reported for the preparation of a variety of α-, β-, γ- and δ-amino acids from 2-pyridone, 2-pyrazinone or 2-hydroxypyrimidine and derivatives The procedure is amenable to scale-up and in most cases no chromatog. purification of the product is required. This approach is useful, especially in the synthesis of amino acids or deuterated amino acids that are not obtained by other methods.

European Journal of Organic Chemistry published new progress about Amino acids Role: SPN (Synthetic Preparation), PREP (Preparation). 25504-47-6 belongs to class piperidines, and the molecular formula is C7H11NO3, Electric Literature of 25504-47-6.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

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>, Related Products of 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 Edition published new progress about Hydrogenation. 25504-47-6 belongs to class piperidines, and the molecular formula is C7H11NO3, Related Products of 25504-47-6.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem