Category: piperazines

Chopin, Nicolas; Yanai, Hikaru; Iikawa, Shinya; Pilet, Guillaume; Bouillon, Jean-Philippe; Medebielle, Maurice published the artcile< A Rapid Entry to Diverse γ-Ylidenetetronate Derivatives through Regioselective -Bromination of Tetronic Acid Derived γ-Lactones and Metal-Catalyzed Postfunctionalization>, Product Details of C16H22N2O3, the main research area is furanone tetronate preparation crystal mol structure.

The synthesis of a series of diverse Me and benzyl γ-ylidenetetronate derivatives was accomplished through the condensation of Me and benzyl tetronates with (hetero)aryl aldehydes in a new two-step or three-step aldolization/dehydration sequence. The bromination of Me and benzyl γ-ylidenetetronates occurred under mild conditions to provide the corresponding C-3-brominated γ-unsaturated lactones. Di- and tribrominated γ-lactones were prepared under slightly different conditions. Some brominated materials were employed in representative Stille, Suzuki-Miyaura , and Sonogashira cross-coupling reactions to yield functionalized Me and benzyl γ-ylidenetetronate derivatives Compounds that resulted from the Sonogashira cross-coupling reactions were desilylated and converted into 1,2,3-triazole derivatives through a copper(I)-catalyzed 1,3-dipolar cycloaddition reaction with benzyl azide. The synthesis of the target compounds was achieved by a reaction of 4-methoxy-2(5H)-furanone (Me tetronate), 4-(phenylmethoxy)-2(5H)-furanone (benzyl tetronate) with aldehydes. The title compounds thus formed included (5Z)-4-methoxy-5-(phenylmethylene)-2(5H)-furanone and related substances.

European Journal of Organic Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Product Details of C16H22N2O3.

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

Allan, Pia N. M.; Ostrowska, Martyna I.; Patel, Bhaven published the artcile< Acetic Acid Catalyzed One-Pot Synthesis of Pyrrolo[1,2- a ]quinoxaline Derivatives>, Safety of 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is pyrroloquinoxaline preparation; benzaldehyde pyrrolylaniline Pictet Spengler reaction acetic acid catalyst.

An efficient acetic acid catalyzed reaction has been developed for the synthesis of 4-aryl substituted pyrrolo[1,2-a]quinoxalines I (R = H, 8-Me, 7-CF3, etc.; Ar = Ph, 2-MeOC6H4, 4-MeC6H4, etc.) from readily available starting materials. A range of structures have been synthesized in very good to excellent yields. The one-pot reaction proceeds through imine formation, cyclization followed by air oxidation

Synlett published new progress about Aromatic heterocyclic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Safety of 1-Boc-4-(4-Formylphenyl)piperazine.

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

Li, Xu; Chen, Xiaolan; Yuan, Jinwei; Qu, Lingbo; Zhu, Haisheng; Bi, Wenzhu; Zhao, Yufen published the artcile< Synthesis and Characterization of Phosphoramide Piperazine Analogs of Paeonol>, COA of Formula: C9H19ClN2O2, the main research area is phosphoramide piperazine analog paeonol preparation.

Based on the phosphorylated reaction, an efficient general synthetic approach that provide facile, rapid and cheap access to a wide range of novel phosphoramide derivatives of paeonol has been developed. These analogs of paeonol are synthesized in high yields and elucidated by IR, HR MS, and NMR.

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Phosphoramides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 76535-74-5 belongs to class piperazines, and the molecular formula is C9H19ClN2O2, COA of Formula: C9H19ClN2O2.

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

De-la-Torre, Pedro; Treuer, Adriana V.; Gutierrez, Margarita; Poblete, Horacio; Alzate-Morales, Jans H.; Trilleras, Jorge; Astudillo-Saavedra, Luis; Caballero, Julio published the artcile< Synthesis and in silico analysis of the quantitative structure-activity relationship of heteroaryl-acrylonitriles as AChE inhibitors>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is AChE inhibitor antiAlzheimers agent mol docking QSAR Alzheimers disease.

Alzheimer disease (AD) is a neurodegenerative disorder that causes damages in brain due to factors such as oxidative stress, low-levels of the neurotransmitter acetylcholine, β-amyloid protein aggregation, etc. It is necessary the design of novel efficient drugs for AD treatment to counteract the increase of people suffering from AD. Recently, heteroaryl-acrylonitrile derivatives have emerged as a new family of acetylcholinesterase inhibitors (AChEIs). The anal. of the structure-activity relationship of these compounds could help to elucidate the main mol. features that contribute to the activity of these compounds In this paper, we performed 3D-QSAR analyses through a Comparative Similarity Indexes Anal. (CoMSIA) to determine the key-factors for the activity of E/Z-heteroaryl-acrylonitriles reported in literature and novel derivatives that are reported in this work for the first time. The novel derivatives were synthesized in order to enlarge the library of compounds available in literature. They were synthesized via microwave-assisted Knoevenagel reaction and their biol. activities as AChE/BuChE inhibitors were explored by the Ellman’s spectrophotometric method. The best CoMSIA model included both electrostatic and hydrogen bond donor fields (CoMSIA-ED model) and provided the best statistical results with a highest Q2 value of 0.901. The model also had satisfactory predictions of external compounds Our in silico study provided a new tool for predicting the affinity of heteroaryl-acrylonitriles as AChEIs to the scientific community. It can be used for guiding the design and synthesis of novel, selective, and more potent AChEIs.

Journal of the Taiwan Institute of Chemical Engineers published new progress about Alzheimer disease. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

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

Jouffroy, Matthieu; Primer, David N.; Molander, Gary A. published the artcile< Base-Free Photoredox/Nickel Dual-Catalytic Cross-Coupling of Ammonium Alkylsilicates>, Computed Properties of 374930-88-8, the main research area is photoredox nickel catalyzed coupling ammonium alkylsilicate hetero aryl bromide.

Single-electron transmetalation is recognized as an enabling technol. for the mild transfer of alkyl groups to transition metal catalysts in cross-coupling reactions. Hypercoordinate silicates represent a new and improved class of radical precursors because of their low oxidation potentials and the innocuous byproducts generated upon oxidation Herein, authors report the cross-coupling of secondary and primary ammonium alkylsilicates with (hetero)aryl bromides in good to excellent yields. The base-free conditions have exceptional protic group tolerance on both partners, permitting the cross-coupling of unprotected primary and secondary amines.

Journal of the American Chemical Society published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent) (hetero). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Computed Properties of 374930-88-8.

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

Khwaja, Sadiya; Fatima, Kaneez; Mishra, Divya; Babu, Vineet; Kumar, Yogesh; Malik, Sumera Banu; Tabassum, Misbah; Luqman, Suaib; Bawankule, Dnyaneshwar U.; Chanda, Debabrata; Khan, Feroz; Mondhe, Dilip M.; Negi, Arvind S. published the artcile< An improved synthesis of indanocine and antiproliferative activity of 2-benzylindanocine via microtubule destabilization>, Quality Control of 197638-83-8, the main research area is colon lung pancreatic cancer indanocine antiproliferative 2benzylindanocine microtubule destabilization; Ehrlich ascites carcinoma; acute oral toxicity; anticancer; antitubulin; indanocine.

Indanocine, a potent anticancer investigational drug of National Cancer Institute-USA, has been much discussed in recent years. Present communication aimed at total synthesis of indanocine and its close analogs. Total synthesis was improved by double yields than previously reported yields. Some of the benzylidene and 2-benzyl derivatives with free rotation at C2 position exhibited potential cytotoxicities against various human cancer cell lines. Five such analogs exhibited potential antiproliferative effect against HCT-116 and MIA PACA-2 cell lines. Benzylindanocine 12i induced microtubule destabilization by occupying colchicine binding pocket of β-tubulin. It also exhibited anti-inflammatory activity by down-regulating IL-6 and TNF-α. In Ehrlich ascites carcinoma model, 12i reduced 78.4% of EAC tumor in Swiss albino mice at 90 mg/kg (i.p.) dose. Further, in in vivo safety studies, 12i was found to be safe to rodents up to 1,000 mg/kg dose. Concomitant anticancer and anti-inflammatory activity of benzylindanocine is distinctive, which suggests its further optimization for better efficacy and druggability.

Chemical Biology & Drug Design published new progress about Antiproliferative agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Quality Control of 197638-83-8.

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

Xie, Fuchun; Zhao, Hongbing; Li, Dewen; Chen, Hong; Quan, Haitian; Shi, Xiaojing; Lou, Liguang; Hu, Youhong published the artcile< Synthesis and Biological Evaluation of 2,4,5-Substituted Pyrimidines as a New Class of Tubulin Polymerization Inhibitors>, Product Details of C11H17BN2O2, the main research area is pyrimidine derivative preparation SAR tubulin polymerization inhibitor antiproliferative activity.

Members of a series of 2,4,5-substituted pyrimidine derivatives were synthesized, and their interactions with tubulin and their antiproliferative activities against the human hepatocellular carcinoma cells of liver (BEL-7402) were evaluated. One member of this family, the indole-pyrimidine I, having an indole-aryl-substituted aminopyrimidine structure, was observed to be an excellent inhibitor of tubulin polymerization (IC50 = 0.79 μM) and to display significantly high antiproliferative activities against several cancer cell lines with IC50 values ranging from 16 to 62 nM. This substance displayed a high propensity to arrests cells at the G2/M phase of the cell cycle (EC50 = 20 nM). In addition, I was found to competitively inhibit colchicine binding to tubulin, indicating that it binds to the colchicine-binding site of tubulin. The observations made in this investigation demonstrate that 2,4,5-substituted pyrimidines represent a new class of tubulin polymerization inhibitors with significant antiproliferative activity.

Journal of Medicinal Chemistry published new progress about Antimitotic agents. 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Product Details of C11H17BN2O2.

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

Liao, Rong; Chang, Yan published the artcile< A study on N-Boc-2,2-dimethyl-piperazine>, Recommanded Product: 3,3-Dimethylpiperazin-2-one, the main research area is dimethylpiperazine synthesis.

This paper studies the reaction temperature, ratio of reactants, and catalyst in order to get N-Boc-2,2-dimethyl-piperazine, a synthesis of ethylenediamine, Et 2-bromoisobutyrate, and di-tert-Bu dicarbonate. Experiment results suggest that the optimal condition is: first, using ethylenediamine and Et 2-bromoisobutyrate with a ratio of 3:1 to get intermediate product under 70°C; and then using the potassium carbonate to catalyze the intermediate product to get the final product.

Sichuan Huagong published new progress about 22476-74-0. 22476-74-0 belongs to class piperazines, and the molecular formula is C6H12N2O, Recommanded Product: 3,3-Dimethylpiperazin-2-one.

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>, Application In Synthesis of 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.

Molecules published 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, Application In Synthesis of 374930-88-8.

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

Rindhe, S. S.; Karale, B. K.; Gupta, R. C.; Rode, M. A. published the artcile< Synthesis, antimicrobial and antioxidant activity of some oxindoles>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is oxindole preparation antibacterial antifungal antioxidant agent; Antibacterial; antifungal and antioxidant activity; oxindole.

The present work describes the synthesis and spectral anal. of several (3Z)-[4-[4-(arylsulfonyl)-1-piperazinyl]benzylidene]-1,3-dihydro-2H-indol-2-one derivatives The title compounds were screened in-vitro against six species of microorganisms, Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Aspergillus clavatus. Most of the compounds exhibited significant antimicrobial activity. All compounds were also screened in-vitro for the antioxidant activity using DPPH assay. Most of them have shown very significant antioxidant activity. The synthesis of the target compounds was achieved by an amidation (sulfonamidation) of 4-[4-[(2-oxo-3-indolylidene)methylene]phenyl]-1-piperazinecarboxylic acid 1,1-dimethylethyl ester with sulfonyl halides. The title compounds thus formed included 1,3-dihydro-3-[(3Z)-[4-[4-[[4-(1-methylethyl)phenyl]sulfonyl]-1-piperazinyl]phenyl]methylene]-2H-indol-2-one (I).

Indian Journal of Pharmaceutical Sciences published new progress about Antibacterial agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

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