Category: piperazines

Yamagishi, Hiroki; Saito, Hayate; Shimokawa, Jun; Yorimitsu, Hideki published the artcile< Design, Synthesis, and Implementation of Sodium Silylsilanolates as Silyl Transfer Reagents>, Application of C13H19BrN4O2, the main research area is sodium silylsilanolate preparation silyl transfer reagent; palladium catalyzed silylation aryl halide pseudohalide sodium silylsilanolate.

There is an increasing demand for facile delivery of silyl groups onto organic bioactive mols. One of the common methods of silylation via a transition-metal-catalyzed coupling reaction employs hydrosilane, disilane, and silylborane as major silicon sources. However, the labile nature of the reagents or harsh reaction conditions sometimes render them inadequate for the purpose. Thus, a more versatile alternative source of silyl groups has been desired. Authors hereby report a design, synthesis, and implementation of storable sodium silylsilanolates that can be used for the silylation of aryl halides and pseudohalides in the presence of a palladium catalyst. The developed method allows a late-stage functionalization of polyfunctionalized compounds with a variety of silyl groups. Mechanistic studies indicate that (1) a nucleophilic silanolate attacks a palladium center to afford a silylsilanolate-coordinated arylpalladium intermediate and (2) a polymeric cluster of silanolate species assists in the intramol. migration of silyl groups, which would promote an efficient transmetalation.

ACS Catalysispublished new progress about Aryl halides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Application of C13H19BrN4O2.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Wang, Xin; Liu, Wei-Gang; Tung, Chen-Ho; Wu, Li-Zhu; Cong, Huan published the artcile< A Monophosphine Ligand Derived from Anthracene Photodimer: Synthetic Applications for Palladium-Catalyzed Coupling Reactions>, Electric Literature of 374930-88-8, the main research area is monophosphine ligand anthracene photodimer preparation coupling catalyst; Miyaura borylation Suzuki couplings heterocyclic electrophile.

Herein, we present an air-stable dianthracenyl monophosphine ligand (diAnthPhos) which can be prepared in two steps from com. available anthracene derivatives The ligand exhibits excellent efficiency for palladium-catalyzed coupling reactions. In particular, Miyaura borylation of heterocycle-containing electrophiles can be facilitated employing the diAnthPhos ligand with a broad substrate scope and low catalyst loading. The valuable synthetic utility of the new ligand is further demonstrated by a one-pot Miyaura borylation/Suzuki coupling protocol for heteroaryl-containing substrates.

Organic Letterspublished new progress about Arylation. 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Electric Literature of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Nishiguchi, Gisele A.; Atallah, Gordana; Bellamacina, Cornelia; Burger, Matthew T.; Ding, Yu; Feucht, Paul H.; Garcia, Pablo D.; Han, Woo-Seok; Klivansky, Liana; Lindvall, Mika published the artcile< Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases>, Computed Properties of 197638-83-8, the main research area is indole pyrazolopyridine derivative preparation SAR Pim kinase inhibitory.

A series of novel 3,5-disubstituted indole e. g., I and pyrazolopyridine e. g., II derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by structure-based drug design, SAR of the series afforded a highly selective indole chemotype that was further developed into a potent set of compounds against Pim-1, 2, and 3 (Pim-1 and Pim-3: IC50 ≤ 2 nM and Pim-2: IC50 ≤ 100 nM).

Bioorganic & Medicinal Chemistry Letterspublished new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Computed Properties of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Benjahad, Abdellah; Benhaddou, Rachida; Granet, Robert; Kaouadji, Mourad; Krausz, Pierre; Piekarski, Salomon; Bosgiraud, Claudine; Delebassee, Sylvie published the artcile< Synthesis and antiretroviral evaluation of 3-alkyl-2-piperazinone nucleoside analogs>, Application In Synthesis of 22476-74-0, the main research area is nucleoside analog synthesis antiretroviral; hydroxypropylpiperazinone glycosidation ribofuranose.

Glycosidation of 3-alkyl N4-(3-hydroxypropyl)-2-piperazinones by protected 1-O-acetyl ribofuranoses produces nucleoside analogs, e.g. I [R = R1 = H, Me; R = (CH2)9Me, R1 = H], in which the base is separated from the sugar by a hydrocarbon spacer arm. The preliminary in vitro test results against retro-viruses seem promising for compounds bearing a long alkyl chain.

Tetrahedron Letterspublished new progress about Antiviral agents. 22476-74-0 belongs to class piperazines, and the molecular formula is C6H12N2O, Application In Synthesis of 22476-74-0.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Kim, Juhyeon; Kim, Yoon Jung; Londhe, Ashwini M.; Pae, Ae Nim; Choo, Hyunah; Kim, Hak Joong; Min, Sun-Joon published the artcile< Synthesis and biological evaluation of disubstituted pyrimidines as selective 5-HT2C agonists>, SDS of cas: 374930-88-8, the main research area is pyrimidine preparation antagonist HT receptor; 5-HT2C receptor; binding affinity; cell-based assay; disubstituted pyrimidine; selectivity.

The synthesis of disubstituted pyrimidine derivatives I [R1 = 3-F, 4-F; n = 0, 1, 2; R2 = piperazin-1-yl, (2R)-2-methylpiperazin-1-yl, 1,4-diazepan-1-yl], II [R3 = (2R)-2-(3-fluorophenyl)propyl, (2R)-2-(4-fluorophenyl)propyl, 3-fluorophenyl, 4-fluorophenyl; R4 = 1,4-diazepan-1-yl, [(3R)-pyrrolidin-3-yl]aminyl, 2,7-diazaspiro[4.4]nonan-2-yl, etc.] and their biol. evaluation as selective 5-HT2C agonists were described. To improve selectivity for 5-HT2C over other subtypes, two series of disubstituted pyrimidines with fluorophenylalkoxy groups at either the 5-position or 4-position and varying cyclic amines at the 2-position were synthesized. The in vitro cell-based assay and binding assay identified compounds II [R3 = (2R)-2-(3-fluorophenyl)propyl, R4 = 1,4-diazepan-1-yl (I); R3 = (2R)-2-(4-fluorophenyl)propyl, R4 = 1,4-diazepan-1-yl] as potent 5-HT2C agonists. Further studies on selectivity to 5-HT subtypes and drug-like properties indicated that 2,4-disubstituted pyrimidine (I) showed a highly agonistic effect on the 5-HT2C receptor, with excellent selectivity, as well as exceptional drug-like properties, including high plasma and microsomal stability, along with low CYP inhibition. Thus, pyrimidine (I) could be considered a viable lead compound as a 5-HT2C selective agonist.

Moleculespublished new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, SDS of cas: 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Cheng, Chuanjie; Sun, Jianwei; Xing, Lixin; Xu, Jimin; Wang, Xinyan; Hu, Yuefei published the artcile< Highly Chemoselective Pd-C Catalytic Hydrodechlorination Leading to the Highly Efficient N-Debenzylation of Benzylamines>, Product Details of C9H19ClN2O2, the main research area is benzylamine debenzylation synergistic trichloroethane chemoselective hydrodechlorination palladium catalyst; amine hydrochloride preparation.

In the presence of 1,1,2-trichloroethane, a novel procedure for the Pd-C catalytic N-debenzylation of benzylamines was established. The method proceeded in a synergistic catalytic system and directly gave the products as crystalline amine hydrochlorides in practically quant. yields.

Journal of Organic Chemistrypublished new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent) (benzylic). 76535-74-5 belongs to class piperazines, and the molecular formula is C9H19ClN2O2, Product Details of C9H19ClN2O2.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Link, Achim; Zhou, Yujing; Buchwald, Stephen L. published the artcile< CuH-Catalyzed Asymmetric Reductive Amidation of α,β-Unsaturated Carboxylic Acids>, Reference of 374930-88-8, the main research area is chiral amide preparation enantioselective amidation carboxylic acid secondary amine.

The direct enantioselective copper hydride (CuH)-catalyzed synthesis of β-chiral amides from α,β-unsaturated carboxylic acids and secondary amines under mild reaction conditions is reported. The method utilizes readily accessible carboxylic acids and tolerates a variety of functional groups in the β-position including several heteroarenes. A subsequent iridium-catalyzed reduction to γ-chiral amines can be performed in the same flask without purification of the intermediate amides.

Organic Letterspublished new progress about Amidation (Reductive). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Reference of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Phelan, James P.; Wiles, Rebecca J.; Lang, Simon B.; Kelly, Christopher B.; Molander, Gary A. published the artcile< Correction: Rapid access to diverse, trifluoromethyl-substituted alkenes using complementary strategies [Erratum to document cited in CA169:178001]>, Electric Literature of 374930-88-8, the main research area is trifluoromethyl alkene preparation erratum; silyl alc trifluoromethyl cross coupling palladium erratum; Peterson elimination erratum; organotrifluoroborate cross coupling palladium erratum.

in the original article the Electronic Supplementary Information footnote included addnl. incorrect CCDC numbers for the crystal data reported; the correction is provided here.

Chemical Sciencepublished new progress about Addition reaction. 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Electric Literature of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Lee, Heajin; Liu, Wenjun; Brown, Adrienne S.; Landgraf, Ralf; Wilson, James N. published the artcile< Fluorescent Kinase Probes Enabling Identification and Dynamic Imaging of HER2(+) Cells>, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid, the main research area is fluorescent kinase probe imaging HER2 cancer.

The human epidermal growth factor receptor, EGFR/ERBB/HER, family of receptor tyrosine kinases is central to many signaling pathways and a validated chemotherapy target in multiple cancers. While EGFR/ERBB-targeted therapies, including monoclonal antibodies, e.g., trastuzumab, and small mol. kinase inhibitors, such as lapatinib, have been developed, rapid identification and classification of cancer cells is key to identifying the best treatment regime. The authors report ERBB2 (also HER2) targeting kinase probes that exhibit a “”turn-on”” emission response upon binding. These live cell compatible probes differentiate ERBB2(+) cells from low-level, ERBB2(-) cells by targeting the intracellular ATP-binding pocket of ERBB2 with therapeutic inhibitor-like specificity. Beyond kinase expression levels, probe signal is linked to the phosphotyrosine-correlated activation state of the ERBB2 population. Addnl., the rapid signaling capability of the probes can report changes in activation state in live cells providing a unique type of complementary information to immunohistochem. assays of receptor kinase populations.

Analytical Chemistry (Washington, DC, United States)published new progress about Confocal laser scanning microscopy. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Recommanded Product: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Jouffroy, Matthieu; Kelly, Christopher B.; Molander, Gary A. published the artcile< Thioetherification via Photoredox/Nickel Dual Catalysis>, Electric Literature of 374930-88-8, the main research area is thioether aryl heteroaryl preparation; aryl heteroaryl bromide thioetherification thiol hypervalent alkylsilicate nickel photoredox.

Hypervalent alkylsilicates represent new and readily accessible precursors for the generation of alkyl radicals under photoredox conditions. Alkyl radicals generated from such silicates serve as effective hydrogen atom abstractors from thiols, furnishing thiyl radicals. The reactive sulfur species generated in this manner can be funneled into a nickel-mediated cross-coupling cycle employing aromatic bromides to furnish thioethers. The serendipitous discovery of this reaction and its utilization for the thioetherification of various aryl and heteroaryl bromides with a diverse array of thiols are described. The S-H selective H atom abstraction event enables a wide range of functional groups, including those bearing protic moieties, to be tolerated.

Organic Letterspublished new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Electric Literature of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics