Category: 300543-56-0

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.300543-56-0,(R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine,as a common compound, the synthetic route is as follows.

General procedure: The title compound was prepared according to General Protocol B. NMR (400 MHz, DMSO-c delta 7.48 – 7.14 (m, 9H), 4.29 (s, 1 H), 2.38 (s, 4H), 2.34 – 2.20 (m, 6H); LCMS ti (Method 1) = 4.630 min, m/z 317.2 [M+H+].General Protocol B. A solution of amine (0.105 mmol) in MeOH (1.00 mL) was treated at room temperature with aldehyde (0.525 mmol to 1.05 mmol, 5.0 to 10.0 equiv.), NaCNBH4 (19.7 mg, 0.315 mmol, 3.0 equiv.) and acetic acid (0.018 mL, 0.315 mmol, 3.0 mmol). The reaction mixture was stirred at room temperature for 1 – 8 h and quenched with 1 N NaOH solution. The mixture was dried by blowing air, re-dissolved in DMSO, filtered and purified by HPLC. The title compound was prepared according to General Protocol B as a TFA salt. LCMS t, (Method 1) = 3.990 min, m/z 445.2 [M+H+]., 300543-56-0

As the paragraph descriping shows that 300543-56-0 is playing an increasingly important role.

Reference：
Patent; THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; LIANG, Tsanyang Jake; FERRER, Marc; HE, Shanshan; HU, Xin; HU, Zongyi; MARUGAN, Juan Jose; SOUTHALL, Noel Terrence; XIAO, Jingbo; ZHENG, Wei; WO2015/80949; (2015); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

300543-56-0, (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step-III: Levorotatory (-)-[2-[4-[(4-Chlorophenyl)-phenylmethyl]-1-piperazinyl]ethanolLevorotatory (-)-1-[(4-chlorophenyl)phenylmethyl]piperazine (50 gm), 2-chloroethanol (31.4 gm), potassium iodide (1.3 gm) and sodium carbonate (40.8 gm) are taken in toluene (446 ml) and refluxed for 24 hours. The reaction mixture is cooled to 25-35 C., washed with water (285 ml) followed by two times with water (each time 185 ml). The layers are separated. Toluene is evaporated from organic layer under reduced pressure to yield 58 gm of levorotatory (-)-[2-[4-[(4-Chlorophenyl)-phenylmethyl]-1-piperazinyl]ethanol.

300543-56-0, 300543-56-0 (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine 668697, apiperazines compound, is more and more widely used in various fields.

Reference：
Patent; SYMED LABS LIMITED; US2009/281318; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

300543-56-0, (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine is a piperazines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

40.0 g of 1-[(R)-(4-chlorophenyl) (phenyl) methyl] piperazine, 14.1 g of sodium hydrogen carbonateAnd a mixture of 78.1 g of N-methyl-2-pyrrolidoneHeat to 120 C, ethyl (2-chloroethoxy) acetateAfter 27.9 g was dropped over 30 minutes, the mixture was stirred for 6 hours.After cooling the obtained suspension to room temperature, 200 g of waterAnd toluene 69gAnd the mixture was separated.120 g of water is added to the obtained organic layer, and liquid separation is performed again to obtain the formula (6).; Example 1 32 g of water was added to a toluene solution of the compound (6) obtained in Reference Example 1, and a solution of 7.0 g of lithium hydroxide monohydrate dissolved in 44 g of water was added dropwise at room temperature. It stirred until it became 0.2% or less. Liquid separation was carried out after the obtained solution, 8 g of N-methyl-2-pyrrolidone for washing, 139 g of toluene and 25 g of acetone were mixed. To the separated aqueous layer were added 139 g of toluene and 13 g of acetone to carry out liquid separation again. Further, 139 g of toluene and 9 g of acetone were added to the separated aqueous layer, and liquid separation was performed again. 35 g of toluene and 193 g of methyl ethyl ketone were added to the obtained aqueous layer, and 29.1 g of 35% hydrochloric acid was dropped to adjust the pH to 2.4, and the solution was heated to 45 C. to separate. After 35 g of toluene was added to the obtained organic layer, concentration was performed until the remaining amount became 95 g. Furthermore, 97 g of methyl ethyl ketone and 35 g of toluene were added and concentrated until the remaining amount reached 99 g, and further 24 g of methyl ethyl ketone and 9 g of toluene were added and concentrated until the remaining amount became 101 g. After adding methyl ethyl ketone 64g and acetone 411g at room temperature and dropping 7.3g of 35% hydrochloric acid,0.04 g of levocetirizine dihydrochloride was added.Subsequently, 316 g of acetone was dropped, and after stirring for 1.5 hours, 6.9 g of 35% hydrochloric acid was dropped. After filtering the obtained suspension, the obtained solid was washed with 95 g of acetone. The obtained crystals were dried under reduced pressure at 40 C. to obtain 54.6 g of levocetirizine dihydrochloride. The purity was 99.8% or more, 300543-56-0

The synthetic route of 300543-56-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sumitomo Chemical Co., Ltd.; Yoshida, Kazuhiro; Ando, Kenichi; (13 pag.)JP2019/43885; (2019); A;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics

Reference of 300543-56-0, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, SMILES is ClC1=CC=C([C@H](N2CCNCC2)C3=CC=CC=C3)C=C1, belongs to piperazines compound. In a article, author is Guo, Shaochen, introduce new discover of the category.

In vitro and in vivo antimicrobial activities of a novel piperazine-containing benzothiazinones candidate TZY-5-84 against Mycobacterium tuberculosis

A piperazine-containing benzothiazinones lead compound PBTZ169, served as DprE1 inhibitor, displays nanomolar bactericidal activity against Mycobacteria tuberculosis. Here, we systematically evaluate anti-tuberculosis activity of one of PBTZ169 analogues, TZY-5-84, in vitro and in vivo. The MIC value of TZY-5-84 against M. tuberculosis H37Rv ranged from 0.014 to 0.015 mg/L, lower than those of INH, RFP and BDQ. Five susceptible and thirteen drug-resistant clinical isolates were also susceptive to TZY-5-84. It had anti-tuberculosis activity against intracellular bacilli in infected macrophage model. It exhibited its activity in time-dependent manner and against intracellular bacilli in infected macrophage cells. However, the MIC of TZY-5-84 against three laboratory PBTZ169-induced resistant isolates increased four-fold increment compared to that of H37Rv. No antagonism was observed in any combination between TZY-5-84 and seven commonly used anti-tuberculosis drugs in an in vitro checkerboard assay. In murine infection model, TZY-5-84 at lower dosage (12.5 mg/kg) was found to be comparatively efficacious as PBTZ169 at 25 mg/kg. Our research suggests TZY-5-84 can be a promising preclinical candidate for further study on TB treatment.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, molecular formula is C17H19ClN2, belongs to piperazines compound. In a document, author is Salaciak, Kinga, introduce the new discover, Product Details of 300543-56-0.

The antidepressant-like activity of chiral xanthone derivatives may be mediated by 5-HT1A receptor and beta-arrestin signalling

Background: Our previous studies showed that xanthone derivatives with N-(2-methoxyphenyl)piperazine fragment have an affinity to the 5-HT1A receptor and show antidepressant-like properties in rodents. In this study, we tested three xanthone derivatives, HBK-1 (R, S) and its enantiomers, in which we increased the distance between the piperazine and xanthone fragments by using a hydroxypropoxy linker. We hypothesized that this would increase the binding to the 5-HT1A receptor and consequently, pharmacological activity. Aims: We aimed to assess the in vitro and in vivo pharmacological activity of the xanthone derivatives. Methods: We evaluated the in vitro affinity for serotonin 5-HT1A and 5-HT2A receptors and serotonin transporter. We also determined the intrinsic activity at the 5-HT1A receptor. We investigated the antidepressant-like properties and safety after acute administration (dose range: 1.25-20 mg/kg) using the forced swim, tail suspension, locomotor activity, rotarod and chimney tests in mice. We also evaluated the basic pharmacokinetic parameters. Results: Our results indicated that the compounds showed a high affinity for the 5-HT1A receptor but very weak antagonistic properties in the Ca2+ mobilization assay; however, they showed significant agonistic properties in the beta-arrestin recruitment assay. In both behavioural tests the studied xanthone derivatives showed antidepressant-like activity. Pre-treatment with p-chlorophenylalanine or WAY-100635 abolished their antidepressant-like activity. None of the compounds caused motor impairments at antidepressant-like doses. The racemate penetrated the blood-brain barrier and had a relatively high bioavailability after intraperitoneal administration. Conclusions: Xanthone derivatives with N-(2-methoxyphenyl)piperazine fragment and hydroxypropoxy linker show increased binding to the 5-HT1A receptor and may represent an attractive putative treatment candidate for depression.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 300543-56-0. Product Details of 300543-56-0.

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

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine. In a document, author is Rolfe, Alan, introducing its new discovery. Name: (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine.

Discovery of 2,6-Dimethylpiperazines as Allosteric Inhibitors of CPS1

Carbamoyl phosphate synthetase 1 (CPS1) is a potential synthetic lethal target in LKB1-deficient nonsmall cell lung cancer, where its overexpression supports the production of pyrimidine synthesis. In other cancer types, CPS1 overexpression and activity may prevent the accumulation of toxic levels of intratumoral ammonia to support tumor growth. Herein we report the discovery of a novel series of potent and selective small-molecule inhibitors of CPS1. Piperazine 2 was initially identified as a promising CPS1 inhibitor through a high-throughput screening effort. Subsequent structure-activity relationship optimization and structure-based drug design led to the discovery of piperazine H3B-616 (25), a potent allosteric inhibitor of CPS1 (IC50 = 66 nM).

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 300543-56-0 help many people in the next few years. Name: (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine.

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

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, SMILES is ClC1=CC=C([C@H](N2CCNCC2)C3=CC=CC=C3)C=C1, in an article , author is Wang, Apeng, once mentioned of 300543-56-0, Category: piperazines.

Design, synthesis and antimycobacterial activity of new benzothiazinones inspired by rifampicin/rifapentine

A series of novel benzothiazinone derivatives containing a N-((methylene)amino)piperazine moiety, inspired by rifampicin/rifapentine, were designed and synthesized. Seven compounds 1a and 1e-j show excellent in vitro activity against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates (MIC: 0.029-0.110 mu M), and accepted selective index (1100 – > 4000). Compound 1h displays good safety and pharmacokinetic profiles, suggesting its promising potential to be lead compound for future antitubercular drug discovery.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, SMILES is ClC1=CC=C([C@H](N2CCNCC2)C3=CC=CC=C3)C=C1, belongs to piperazines compound. In a document, author is Gao, Zhuo Fan, introduce the new discover, Safety of (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine.

Selection of crosslinkers and control of microstructure of vapor-phase crosslinked composite membranes for organic solvent nanofiltration

A fast and green chemical modification method has been developed by using amine vapor to fabricate hybrid composite membranes consisting of crosslinked polyimides and nano-size UiO-66-NH2 metal-organic frameworks (MOFs) with higher selectivity for organic solvent nanofiltration (OSN). Three amine vapor-phase crosslinking (VPC) reagents; namely, N,N’-Bis(3-aminopropyl)-1,3-propanediamine (APPD), 1,4-Bis(3-aminopropyl) piperazine (BAPP) and polyethylenimine (PEI) were employed. It was found that APPD and PEI vapor are more effective to generate smaller pores in the dense-selective layer than the BAPP vapor. In addition, the PEI modified membranes are more suitable for polar and aprotic solvents nanofiltration applications, while the APPD and BAPP modified membranes are for applications involving wider solvents. The selected hybrid membranes cast on polyester (PET) non-woven fabrics have rejections of tetracycline (MW = 444 gmol(-1)) more than 90% in four organic solvents under continuous cross-flow filtration tests for over 120 h. All fluxes and selectivities remain stable without showing significant fluctuations, evidencing great potentials of designed membranes for industrial applications. Besides, the VPC modification process is environmental-friendly because it uses a tiny amount of amine vapors without extra chemical waste production. Therefore, this study offers a promising sustainable, greener and scalable strategy to produce high performance OSN membranes.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 300543-56-0 is helpful to your research. Safety of (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine.

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

In an article, author is Mazzotta, Sarah, once mentioned the application of 300543-56-0, Computed Properties of C17H19ClN2, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, molecular formula is C17H19ClN2, molecular weight is 286.8, MDL number is MFCD11519277, category is piperazines. Now introduce a scientific discovery about this category.

Exploration of piperazine-derived thioureas as antibacterial and anti-inflammatory agents. In vitro evaluation against clinical isolates of colistin-resistant Acinetobacter baumannii

A. baumannii is one of the most important multidrug-resistant microorganisms in hospital units. It is resistant to many classes of antibiotics and the development of new therapeutic strategies is necessary. The aim of this study was to evaluate the antibacterial activity of a set of piperazine-derived thioureas against 13 clinical strains of colistin-resistant A. baumannii. Six derivatives were identified to inhibit bacterial growth of 46% of the A. baumannii strains at low micromolar concentrations (Minimum Inhibitory Concentration from 1.56 to 6.25 mu M). A common structural feature in most active compounds was the presence of a 3,5-bis-trifluoromethyl phenyl ring at the thiourea function. In addition, the ability of the compounds to inhibit production of nitric oxide (NO) was examined in RAW 264.7 murine macrophages, highlighting the potential of piperazine-derived thioureas as promising scaffolds for the design of new combined anti-bacterial/anti-inflammatory agents.

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

Related Products of 300543-56-0, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 300543-56-0, Name is (R)-1-((4-Chlorophenyl)(phenyl)methyl)piperazine, SMILES is ClC1=CC=C([C@H](N2CCNCC2)C3=CC=CC=C3)C=C1, belongs to piperazines compound. In a article, author is Ju, Xiaohui, introduce new discover of the category.

Electrospun transition layer that enhances the structure and performance of thin-film nanofibrous composite membranes

Electrospun nanofibers with completely interconnected pore structures are increasingly considered as substrates for fabricating thin-film nanofibmus composite (TFNC) nanofiltration (NF) membranes. The poor adhesion between the large-pore substrate and dense selective layer has been considered as the bottleneck for wide application. This work presents the role of a transition layer on membrane structure as well as performance enhancement. Specifically, both polyethyleneimine (PEI)/polyacrylonitrile (PAN) transition layer and PAN substrate layer are formed by electrospinning. Interfacial polymerization (IP) is subsequently performed with trimesoyl chloride and piperazine. The introduction of the PEI modified transition layer improves the hydrophilicity, provides additional reaction sites for IP, and avoids the polymerization in the pores of nanofibers. The resultant composite NF membranes exhibit a compact and defect-free selective layer. Such an optimal structure leads to an excellent separation performance of 95.6% for orange II dye (MW = 350.32 g/mol) rejection and 38.5 L m(-2)h(-1) bar -1 for the pure water permeability. It exhibits stable long-term performance during low pressure (0.2 MPa) nanofiltration, which will afford significant directions for the actual application of the TFNC membranes in water purification and other fields.

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