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Journal articles on the topic 'Piperazina'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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1

DEMUNER, Antônio Jacinto, Mauro LONGUE FILHO, Luiz Cláudio de Almeida BARBOSA, and Maria Amélia dos SANTOS. "Sintese e avaliação da atividade nematicida de derivados da piperazina." Eclética Química 26 (2001): 11–24. http://dx.doi.org/10.1590/s0100-46702001000100001.

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Na busca de novos nematicidas sintéticos, oito derivados da piperazina foram preparados. Esses compostos, e também dois derivados da piperazina e a piperazina, disponíveis comercialmente, foram submetidos a ensaios biológicos para avaliar a atividade dos mesmos sobre os fitonematóides Meloidogyne incognita e Heterodera glycines. Na concentração de 20 mig mL-1, os compostos causaram de 3 a 73% de mortalidade em M. incognita e de 7 a 58% de mortalidade em H. glycines.

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2

Kmoníček, Vojtěch, Martin Valchář, and Zdeněk Polívka. "Some 4-Substituted 1-(3-Pyridylmethyl)piperazines with Antihistamine Activity." Collection of Czechoslovak Chemical Communications 59, no. 10 (1994): 2343–50. http://dx.doi.org/10.1135/cccc19942343.

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Several compounds derived from nicotinic acid were prepared within a more extensive programme aiming at the synthesis of new substances with expected antihistamine and antidepressant activity. Some of these compounds display certain structural resemblance with the antidepressant agent piberaline (EGYT 475, Trelibet®, I) and its analogues. The products were used as intermediates for the synthesis of further compounds and most of them were subjected to pharmacological testing. Substituted nicotinic acid piperazides IIa - IId and IVa - IVe were obtained by reactions of nicotinoyl chloride (prepar

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3

Gettys, Kristen, Zhishi Ye, and Mingji Dai. "Recent Advances in Piperazine Synthesis." Synthesis 49, no. 12 (2017): 2589–604. http://dx.doi.org/10.1055/s-0036-1589491.

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Piperazine ranks as the third most common N-heterocycle appearing in small-molecule pharmaceuticals. This review highlights recent advances in methods development for the construction of the piperazine ring system with particular emphasis on preparing carbon-substituted piperazines.1 Introduction2 Reduction of (Di)ketopiperazine3 N-Alkylation4 Transition-Metal-Catalyzed/Mediated Piperazine Synthesis4.1 The SnAP and SLAP Methods4.2 Palladium-Catalyzed Cyclization4.3 Gold-Catalyzed Cyclization4.4 Other Metal-Catalyzed/Mediated Cyclization4.5 Borrowing Hydrogen Strategy4.6 Imine Reductive Cycliz

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4

Chagas, N. A., and M. Mascarenhas. "Efeitos Neurobiológicos do Uso de 1-(3-clorofenil) Piperazina." Ciência em Movimento - Biociências e Saúde 15, no. 30 (2013): 27–34. http://dx.doi.org/10.15602/1983-9480/cmbs.v15n30p27-34.

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5

Yadav, Pradeep, and Y. C. Joshi. "Synthesis and Spectral Study of Novel Norfloxacin Derivatives." E-Journal of Chemistry 5, s2 (2008): 1154–58. http://dx.doi.org/10.1155/2008/357073.

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Reaction of [1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinolone-3-carboxylic acid (norfloxacin) with thiazole / benzothiazole diazonium chloride to get new piperazine substituted norfloxacin derivative. These norfloxacin derivatives were further condensed with variousβ-diketone to get novel acid derivatives of 1-Ethyl-6-fluoro-4-oxo-7- [4 (thiazol-2-yldiazenyl)-piperzin-1-yl]-1,4-dihydro-quinoline-3-carboxylic acid (6a-e) and 7-(4-(benzo[d]thiazol-2-yldiazenyl)piperazin-1-yl)-1-ethyl-6-fluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (6 f-j). Structures of these compounds were

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6

Kafka, Stanislav, Jan Čermák, Tomáš Novák, František Pudil, Ivan Víden, and Miloslav Ferles. "Syntheses of piperazines substituted on the nitrogen atoms with allyl, propyl, 2-hydroxypropyl and 3-hydroxypropyl groups." Collection of Czechoslovak Chemical Communications 50, no. 5 (1985): 1201–11. http://dx.doi.org/10.1135/cccc19851201.

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The paper describes synthesis of 1,4-diallylpiperazine (I), 1-allylpiperazine (III), 1-propylpiperazine (IV), 1-(1-piperazinyl)-2-propanol (V), 3-(1-piperazinyl)-1-propanol (VI), 1-allyl-4-propylpiperazine (VII), 1-(4-allyl-1-piperazinyl)-2-propanol (VIII), 3-(4-allyl-1-piperazinyl)-1-propanol (IX), 1,4-dipropylpiperazine (X), 1-(4-propyl-1-piperazinyl)-2-propanol (XI), 3-(4-propyl-1-piperazinyl)-1-propanol (XII), 1,4-bis(2-hydroxypropyl)piperazine (XIII), 3-[4-(2-hydroxypropyl)-1-piperazinyl]-1-propanol (XIV) and 1,4-bis(3-hydroxypropyl)piperazine (XV). Retention indices of I-XV reported and

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7

Jílek, Jiří, Martin Valchář, Jiří Holubek, et al. "Noncataleptic neuroleptic agents: 2-(4-(2-(2-Chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yloxy)ethyl)piperazine-1-yl)ethanol and some related compounds." Collection of Czechoslovak Chemical Communications 53, no. 11 (1988): 2731–41. http://dx.doi.org/10.1135/cccc19882731.

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10-(2-Bromoethoxy)-2-chloro-10,11-dihydrodibenzo[b,f]thiepin (X), prepared by two methods, was subjected to substitution reactions with 2-(1-piperazinyl)ethanol, 3-(1-piperazinyl)propanol, 1-methylpiperazine, 3-(1-piperazinyl)propionamide, piperazine, and 1-(ethoxycarbonyl)piperazine and gave the title compounds II-VII. The alcohol II was esterified by treatment with acid chlorides to compounds VIII and IX. Compounds II, V, and VIII proved to be noncataleptic neuroleptic agents and II (clopithepin, VÚFB-17 076) was selected for preclinical studies.

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8

Little, Vanessa Renee, and Keith Vaughan. "Synthesis and characterization of several series of 4-acyl-1-[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 92, no. 9 (2014): 838–48. http://dx.doi.org/10.1139/cjc-2014-0242.

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Five series of a novel class of 4-acyl-1-[2-aryl-1-diazenyl]piperazines have been synthesized and characterized: the 4-acetyl-1-[2-aryl-1-diazenyl]piperazines [series 1]; the 4-cyclohexylcarbonyl-1-[2-aryl-1-diazenyl]piperazines [series 2]; the 4-benzoyl-1-[2-aryl-1-diazenyl]piperazines [series 3]; the benzyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 4]; and the t-butyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 5]. The compounds were synthesized by diazotization of a primary aromatic amine and subsequent coupling to an appropriate secondary amine: 1-acetylpiperazine [

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9

Schmitz, Ana Paula, Olyr Celestino Kreutz, and Edna Sayuri Suyenaga. "ANTIPSICÓTICOS ATÍPICOS VERSUS EFEITO OBESOGÊNICO SOB A ÓPTICA DA QUÍMICA MEDICINAL." Revista Eletrônica de Farmácia 12, no. 3 (2015): 23. http://dx.doi.org/10.5216/ref.v12i3.33714.

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Os fármacos antipsicóticos são os principais agentes utilizados no tratamento da esquizofrenia e atuam principalmente como antagonistas do receptor dopaminérgico D2. Entre eles, destacam-se os antipsicóticos atípicos, os quais apresentam um perfil farmacológico peculiar por induzirem menos efeitos extrapiramidais. Geralmente são indicados aos pacientes com sintomas negativos da esquizofrenia, ou em casos refratários ao tratamento com medicamentos de primeira geração, porém são relatados . Desta forma, foi realizada uma revisão bibliográfica sobre estes fármacos correlacionando a estrutura quím

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10

Song, Yanxi, C. S. Chidan Kumar, G. B. Nethravathi, S. Naveen, and Hongqi Li. "Cinnarizinium picrate." Acta Crystallographica Section E Structure Reports Online 68, no. 6 (2012): o1747. http://dx.doi.org/10.1107/s1600536812020764.

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In the title salt {systematic name: 4-diphenylmethyl-1-[(E)-3-phenylprop-2-en-1-yl]piperazin-1-ium 2,4,6-trinitrophenolate), C26H29N2 +·C6H2N3O7 −, the cinnarizinium cation is protonated at the piperazine N atom connected to the styrenylmethyl group; the piperazine ring adopts a distorted chair conformaiton. In the crystal, bifurcated N—H...(O,O) hydrogen bonds link the components into two-ion aggregates.

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11

Nivedita Desai, R., S. Sreenivasa, S. Naveen, N. K. Lokanath, P. A. Suchetan, and D. B. Aruna Kumar. "Crystal structure of 2-(4-methylpiperazin-1-yl)quinoline-3-carbaldehyde." Acta Crystallographica Section E Crystallographic Communications 71, no. 11 (2015): o900—o901. http://dx.doi.org/10.1107/s2056989015020186.

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In the title compound, C15H17N3O, the aldehyde group is twisted relative to the quinoline group by17.6 (2)° due to the presence of a bulky piperazinyl group in theorthoposition. The piperazine N atom attached to the aromatic ring issp3-hybridized and the dihedral angle between the mean planes through the the six piperazine ring atoms and through the quinoline ring system is 40.59 (7)°. Both piperazine substituents are in equatorial positions.

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12

O’Malley, Karen, and Keith Vaughan. "Synthesis and Characterization of a Series of 1-Aryl-4-[Aryldiazenyl]-piperazines. Part II1. 1-Aryl-4-(2-Aryl-1-Diazenyl)-piperazines with Fluoro-, chloro-, Methyl-, Cyano- and Acetyl Substituents in The 1-Aryl Group." Open Chemistry Journal 3, no. 1 (2016): 42–55. http://dx.doi.org/10.2174/1874842201603010042.

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This paper reports the synthesis and characterization of eight series of 1-aryl-4-(2-aryl-1-diazenyl)-piperazines (12 to 19). Several series of these triazenes have been synthesized by the diazotization of a primary arylamine followed by diazonium coupling with a secondary arylpiperazine . The arylpiperazines used in this study are: 1-phenylpiperazine, 1-(4-fluorophenyl-)piperazine, 1-(4-chlorophenyl-)piperazine, 1-(3,4-dichlorophenyl-)piperazine, 1-(2-methylphenyl-)-piperazine, 1-(4-acetophenyl-)-piperazine, 1-(2-pyridyl-)piperazine and 2-cyanophenylpiperazine. These new triazenes (series 12-

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13

Prabawati, Susy Yunita. "SYNTHESIS OF 1,4-BIS [(1-HYDROXY-4-T-BUTYL-PHENYL) METHYL]PIPERAZINE AS ANTIOXIDANTS." Molekul 11, no. 2 (2016): 220. http://dx.doi.org/10.20884/1.jm.2016.11.2.244.

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A study has been conducted to synthesize 1,4-bis [(1-hydroxy-4-t-butyl-phenyl)-methyl]piperazin using phenol derivate and investigate the capability of that compound, as an antioxidant. The synthesis was carried out through Mannich reaction using p-t-butylphenol, paraformaldehyde, and piperazine. The product was characterized by IR and 1H NMR spectroscopic. Testing of antioxidant activity was done with the immersion of DPPH (1,1-diphenyl-2 picrylhydrazyl) free radical method. The product was obtained as a white solid, with a point of 252,7-254,7 ºC and a yield of 65.76%. The test of antioxidan

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14

González Garcia, Filiberto, Eduardo Miguez, and Maria Inês B. Tavares. "Caracterización cualitativa de poliaminas libres en endurecedores de resinas epoxídicas del tipo etilenaminas por espectroscopia de resonancia magnética nuclear." Polímeros 18, no. 1 (2008): 45–51. http://dx.doi.org/10.1590/s0104-14282008000100010.

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La caracterización cualitativa de dos agentes de curado comerciales de resinas epoxídicas del tipo etilenaminas comercializados por la ACROS (U.S.A.) fue realizada usando la espectroscopia de resonancia magnética nuclear de carbono-13. Los productos comerciales corresponden a la trietilentetramina (TETA) y a la tetraetilenpentamina (TEPA). El producto TETA presentó cuatro compuestos diferentes. El compuesto mayoritario correspondió a la trietilentetramina en una concentración de 60% molar que corresponde a una etilenamina de estructura linear. Los otros tres compuestos, uno de ellos mostró est

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15

Penjisevic, Jelena, Vladimir Sukalovic, Deana Andric, et al. "Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines." Journal of the Serbian Chemical Society 81, no. 4 (2016): 347–56. http://dx.doi.org/10.2298/jsc151021097p.

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A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates 1-(2-methoxyphenyl)-4-(piperidin-4-yl)piperazine and 1-(2-methoxyphenyl)-4-(piperidin-4-ylmethyl)piperazine. Biological evaluation of the synthesized compounds was pointed out for seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl)piperidin-4-yl]methyl}piperazine had the highest affinity for the dopamine D2 receptor. For all seven selected compounds docking analysis was performed in order to establish their structure-to-activity relationship.

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16

Al-Soud, Yaseen, Najim Al-Masoudi, Hamed Hassan, Erik De Clercq, and Christophe Pannecouque. "Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives." Acta Pharmaceutica 57, no. 4 (2007): 379–93. http://dx.doi.org/10.2478/v10007-007-0031-7.

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Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivativesA series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H- -imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and alkyl- [4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin- -1-yl)ketones (11-20) as well as the indole analogue22were synthesized from 4-nitro-5-piperazinyl imidazole derivative1, with the aim to develop newly non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound2showed i

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17

Magriotis, Plato A. "Recent progress toward the asymmetric synthesis of carbon-substituted piperazine pharmacophores and oxidative related heterocycles." RSC Medicinal Chemistry 11, no. 7 (2020): 745–59. http://dx.doi.org/10.1039/d0md00053a.

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The piperazine drugs are mostly N-substituted compared to only a few C-substituted drugs. To explore this unknown chemical space, asymmetric syntheses of C-substituted piperazines is the subject of this review.

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18

Kiran Kumar, Haruvegowda, Hemmige S. Yathirajan, Belakavadi K. Sagar, Sabine Foro, and Christopher Glidewell. "Six 1-aroyl-4-(4-methoxyphenyl)piperazines: similar molecular structures but different patterns of supramolecular assembly." Acta Crystallographica Section E Crystallographic Communications 75, no. 8 (2019): 1253–60. http://dx.doi.org/10.1107/s2056989019010491.

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Six new 1-aroyl-4-(4-methoxyphenyl)piperazines have been prepared, using coupling reactions between benzoic acids and N-(4-methoxyphenyl)piperazine. There are no significant hydrogen bonds in the structure of 1-benzoyl-4-(4-methoxyphenyl)piperazine, C18H20N2O2, (I). The molecules of 1-(2-fluorobenzoyl)-4-(4-methoxyphenyl)piperazine, C18H19FN2O2, (II), are linked by two C—H...O hydrogen bonds to form chains of rings, which are linked into sheets by an aromatic π–π stacking interaction. 1-(2-Chlorobenzoyl)-4-(4-methoxyphenyl)piperazine, C18H19ClN2O2, (III), 1-(2-bromobenzoyl)-4-(4-methoxyphenyl)

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19

González Garcia, Filiberto, Maria E. Leyva, Alvaro A. A. de Queiroz, and Olga Higa. "Novas tendências dos polímeros epoxídicos: propriedades biológicas in vitro de formulações para aplicações médicas." Polímeros 19, no. 3 (2009): 177–82. http://dx.doi.org/10.1590/s0104-14282009000300004.

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Este trabalho descreve as propriedades biológicas in vitro de três formulações epoxídicas usando o monômero do tipo éter diglicidílico do bisphenol-A (DGEBA) com três co-monômeros do tipo poliamina alifática de maneira independente; trietilenotetramina (TETA), 1-(2-aminoetil)piperazina (AEP) e isoforonodiamina (IPD). As interações biológicas entre os polímeros obtidos e o sangue foram estudadas in vitro utilizando quatro métodos biológicos diferentes. Estudos de adsorção protéica, adesão plaquetária, formação de trombos e citotoxicidade são apresentados e discutidos. Os ensaios de adsorção pro

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20

Little, Vanessa Renée, Reid Tingley, and Keith Vaughan. "Triazene derivatives of (1,x)-diazacycloalkanes. Part III. Synthesis and characterization of a series of 1,4-di[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 83, no. 5 (2005): 471–76. http://dx.doi.org/10.1139/v05-064.

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Reaction of a series of diazonium salts with piperazine in a 2:1 molar ratio affords excellent yields of the 1,4-di-[2-aryl-1-diazenyl]piperazines (3), which have been characterized by IR and NMR spectroscopy. Structural characterization is supported by elemental analysis or by mass spectrometry with accurate mass measurement of the molecular ion. The protons of the piperazine ring hydrogens give rise to a sharp singlet at ca. 4 ppm in the NMR spectra, indicating that the conformational equilibrium in the piperazine ring is rapid on the NMR timescale. The four equivalent carbon atoms of the pi

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21

Kavitha, Channappa N., Manpreet Kaur, Brian J. Anderson, Jerry P. Jasinski, and H. S. Yathirajan. "1-Piperonylpiperazinium 4-chlorobenzoate." Acta Crystallographica Section E Structure Reports Online 70, no. 3 (2014): o283—o284. http://dx.doi.org/10.1107/s1600536814002037.

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In the title salt {systematic name: 1-[(1,3-benzodioxol-5-yl)methyl]piperazin-1-ium 4-chlorobenzoate}, C12H17N2O2+·C7H4ClO2−, the piperazine ring adopts a slightly disordered chair conformation. The dioxole ring is in a flattened envelope conformation with the methylene C atom forming the flap. The relative orientation of the piperonyl ring system and the piperazine rings is reflected in the N—C—C...;C torsion angle of 132.3 (1)°. In the anion, the mean plane of the carboxylate group is twisted from that of the benzene ring by 14.8 (9)°. In the crystal, the components are linked by N—H...O and

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22

Hakimi, Mohammad, Zahra Mardani, Keyvan Moeini, Esther Schuh, and Fabian Mohr. "A Spectral and Structural Study of the New Cadmium Salt [(H2L)2][Cd2I6][(NO3)2]." Zeitschrift für Naturforschung B 68, no. 3 (2013): 272–76. http://dx.doi.org/10.5560/znb.2013-2295.

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The reaction between 2-(piperazin-1-yl)ethanol and cyclohexene oxide under microwave irradiation gave 2-(4-(2-hydroxyethyl)piperazin-1-yl)cyclohexanol (L). The new cadmium salt [(H2L)2][Cd2I6][(NO3)2] (1) was prepared from the reaction of cadmium iodide with L and identified by elemental analysis, FT-IR and Raman spectroscopy, and single-crystal X-ray diffraction. In the crystal structure of 1, there is a [Cd2I6]2- dianion with distorted tetrahedral geometry for each cadmium atom. The piperazine and cyclohexane rings in 1 have a chair conformation. In the crystal there are several intermolecul

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23

González Garcia, F., F. Matusalém, M. E. Leyva, and A. A. A. Queiroz. "Determinação da massa equivalente de hidrogênio amina em endurecedores do tipo amina alifática por titulação potenciométrica." Matéria (Rio de Janeiro) 15, no. 1 (2010): 70–75. http://dx.doi.org/10.1590/s1517-70762010000100009.

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Um conjunto de endurecedores de resinas epoxídicas do tipo aminas alifáticas foram caracterizados por titulação potenciométrica. Os endurecedores correspondem a compostos de cadeia linear: etilenoamina (EDA), dietilenotriamina (DETA), trietilenotetramina (TETA), tetraetilenopentamina (TEPA), e compostos de cadeia cíclica: 1-(2-aminoetil)piperazina (AEP), isoforondiamina (IPD) e 4,4-diamino-3,3’-dimetilciclohexilmetano (3DCM). Determinou-se a massa equivalente de hidrogênio amina (MEHA) de cada composto de modo indireto por reação de protonação dos nitrogênios do tipo amina utilizando-se soluçã

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24

Dileep, Kommula, and M. Murty. "Aqueous, One-Pot, Three-Component Reaction for Efficient Synthesis of 2-[4-(Arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, ‑1H-benzimidazole, or -1,3-benzoxazole Derivatives." Synlett 28, no. 17 (2017): 2295–98. http://dx.doi.org/10.1055/s-0036-1590972.

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A simple and efficient synthetic protocol has been developed involving a one-pot three-component reaction of a 2-chlorobenzazole, piperazine, and an arenesulfonyl chloride under aqueous conditions at room temperature in the absence of a catalyst, ligand, or base. By using this protocol, a variety of 2-[4-(arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, -1H-benzimidazole, and -1,3-benzoxazole derivatives were synthesized in excellent yields.

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25

Němečková, Dana, Eva Havránková, Jan Šimbera, Richard Ševčík, and Pavel Pazdera. "Simplified Procedure for General Synthesis of Monosubstituted Piperazines—From a Batch Reaction Vessel to a Flow (Microwave) Reactor." Molecules 25, no. 9 (2020): 2168. http://dx.doi.org/10.3390/molecules25092168.

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We reported a novel simplified synthetic procedure for the preparation of monosubstituted piperazine derivatives which can now be easily prepared in a one-pot-one-step way from a protonated piperazine with no need of introduction of a protecting group. Reactions, proceeding either at room or higher temperatures in common solvents, involve heterogeneous catalysis by metal ions supported on commercial polymeric resins. A general synthetic scheme was successfully applied to afford a wide range of monosubstituted piperazines. Furthermore, we picked up a set of piperazine derivatives and studied th

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26

Ye, Zhishi, Kristen E. Gettys, and Mingji Dai. "Opportunities and challenges for direct C–H functionalization of piperazines." Beilstein Journal of Organic Chemistry 12 (April 13, 2016): 702–15. http://dx.doi.org/10.3762/bjoc.12.70.

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Piperazine ranks within the top three most utilized N-heterocyclic moieties in FDA-approved small-molecule pharmaceuticals. Herein we summarize the current synthetic methods available to perform C–H functionalization on piperazines in order to lend structural diversity to this privileged drug scaffold. Multiple approaches such as those involving α-lithiation trapping, transition-metal-catalyzed α-C–H functionalizations, and photoredox catalysis are discussed. We also highlight the difficulties experienced when successful methods for α-C–H functionalization of acyclic amines and saturated mono-

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27

Garcia, F. G., F. Matusalém, M. E. Leyva, A. A. A. Queiroz, and M. G. Oliveira. "Material compósito epóxi-amina para restauração dentária." Matéria (Rio de Janeiro) 14, no. 4 (2009): 1154–61. http://dx.doi.org/10.1590/s1517-70762009000400008.

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O objetivo deste trabalho foi desenvolver materiais compósitos à base de resina epoxídica para restauração dentária, para uso em próteses fixas. Diferentes compósitos foram formulados utilizando a resina líquida do tipo éter diglicidílico do bisfenol-A (DGEBA), com três diferentes agentes de cura tais como trietilenotetramina (TETA), isoforonodiamina (IPD) e 1-(2-aminoetil)piperazina (AEP), como sistemas independentes, contendo diferentes concentrações de micro-partículas de quartzo. As formulações foram otimizadas usando métodos de titulação de grupos funcionais, bem como a incorporação de di

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28

Wierschem, Frank, and Karola Rück-Braun. "Introduction of Substituents on the 2-Oxo-piperazine Skeleton by [3+2] Cycloaddition and Subsequent Transformation." Zeitschrift für Naturforschung B 61, no. 4 (2006): 431–36. http://dx.doi.org/10.1515/znb-2006-0410.

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The 3,4-substituted 2-oxo-piperazines 5 - 9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,3-aminoalcohols with a 3,4-substituted 2-oxo-piperazine scaffold is briefly discussed for adducts derived from N-substituted maleic imides

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29

Zhang, Gang, and Courtney C. Aldrich. "Macozinone: revised synthesis and crystal structure of a promising new drug for treating drug-sensitive and drug-resistant tuberculosis." Acta Crystallographica Section C Structural Chemistry 75, no. 8 (2019): 1031–35. http://dx.doi.org/10.1107/s2053229619009185.

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Mycobacterium tuberculosis (Mtb), the principal etiological agent of tuberculosis (TB), infects over one-quarter of humanity and is now the leading cause of infectious disease mortality by a single pathogen. Macozinone {2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one, C20H23F3N4O3S} is a promising new drug for treating drug-sensitive and drug-resistant TB that has successfully completed phase I clinical trials. We report the complete spectroscopic and structural characterization by 1H NMR, 13C NMR, HRMS, IR, and X-ray crystallography. The cyclohexyl

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30

Ullah, Nisar. "Synthesis of New 1-Aryl-4-(biarylmethylene)piperazine Ligands, Structurally Related to Adoprazine (SLV313)." Zeitschrift für Naturforschung B 67, no. 1 (2012): 75–84. http://dx.doi.org/10.1515/znb-2012-0113.

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A series of new 1-aryl-4-(biarylmethylene)piperazines has been synthesized. These ligands are structurally related to SLV-313, a potential atypical antipsychotic having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halides and subsequent removal of the boc group rendered arylpiperazines. The reductive amination of the latter with suitable biarylaldehydes accomplished the synthesis of these ligands.

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31

Harish Chinthal, Chayanna, Channappa N. Kavitha, Hemmige S. Yathirajan, Sabine Foro, and Christopher Glidewell. "Six 1-halobenzoyl-4-(2-methoxyphenyl)piperazines having Z′ values of one, two or four; disorder, pseudosymmetry, twinning and supramolecular assembly in one, two or three dimensions." Acta Crystallographica Section E Crystallographic Communications 77, no. 1 (2021): 5–13. http://dx.doi.org/10.1107/s2056989020015649.

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Six 1-halobenzoyl-4-(2-methoxyphenyl)piperazines have been prepared using carbodiimide-mediated coupling reactions between halobenzoic acids and N-(2-methoxyphenyl)piperazine. The molecules of 1-(4-fluorobenzoyl)-4-(2-methoxyphenyl)piperazine, C18H19FN2O2 (I), are linked into a chain of rings by a combination of C—H...O and C—H...π(arene) hydrogen bonds. 1-(4-Chlorobenzoyl)-4-(2-methoxyphenyl)piperazine, C18H19ClN2O2 (II), crystallizes in the space group Pca21 with Z′ = 4 and it exhibits both pseudosymmetry and inversion twinning: a combination of six C—H...O and two C—H...π(arene) hydrogen bo

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32

Kurteva, Vanya B., Boris L. Shivachev, and Rositsa P. Nikolova. "Spontaneous conversion of O -tosylates of 2-(piperazin-1-yl)ethanols into chlorides during classical tosylation procedure." Royal Society Open Science 6, no. 2 (2019): 181840. http://dx.doi.org/10.1098/rsos.181840.

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A direct conversion of piperazinyl ethanols into chlorides via a classical O -tosylation protocol is observed. The acceleration of the transformation by the piperazine unit is demonstrated. It is found that the reaction goes via the corresponding O -tosylate, which converts spontaneously into chloride with different rate depending on the substrate structure. In the case of pirlindole derivative, partially aromatized chloride formation was observed upon prolongation and/or increased excess of tosyl chloride.

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33

Song, Yanxi, C. S. Chidan Kumar, S. Chandraju, S. Naveen, and Hongqi Li. "4-[(4-Chlorophenyl)(phenyl)methyl]piperazin-1-ium picrate monohydrate." Acta Crystallographica Section E Structure Reports Online 68, no. 8 (2012): o2486. http://dx.doi.org/10.1107/s1600536812031984.

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The asymmetric unit of the title compound, C17H20ClN2+·C6H2N3O7−·H2O, contains a piperazin-1-ium cation, a picrate anion and one solvent water molecule. The piperazene ring is protonated at one N atom and adopts a highly distorted chair conformation with the chloropheny(phenyl)methyl substituent on the second N atom in an equatorial position. The crystal structure is stabilized by O—H...O, N—H...O and C—H...O hydrogen bonds.

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34

Thamban Chandrika, Nishad, Sanjib K. Shrestha, Huy X. Ngo, Oleg V. Tsodikov, Kaitlind C. Howard, and Sylvie Garneau-Tsodikova. "Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents." Journal of Medicinal Chemistry 61, no. 1 (2017): 158–73. http://dx.doi.org/10.1021/acs.jmedchem.7b01138.

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35

Cai, Dong, ZhiHua Zhang, Yufan Meng та ін. "Efficient synthesis of piperazinyl amides of 18β-glycyrrhetinic acid". Beilstein Journal of Organic Chemistry 16 (21 квітня 2020): 798–808. http://dx.doi.org/10.3762/bjoc.16.73.

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In the present study, a practical method to prepare piperazinyl amides of 18β-glycyrrhetinic acid was developed. Two main procedures for the construction of important intermediate 8 are discussed. One procedure involves the amidation of 1-Boc-piperazine with 3-acetyl-18β-glycyrrhetinic acid, prepared by the reaction of 18β-glycyrrhetinic acid with acetic anhydride without any solvent at 130 °C. The other procedure to prepare compound 8 involves the amidation of 18β-glycyrrhetinic acid followed by the esterification with acetic anhydride. Finally, compound 8 underwent N-Boc deprotection to prep

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36

Hulinská, Hana, Zdeněk Polívka, Jiří Jílek, et al. "Experimental antiulcer agents: N-substituted 2-(4-methyl-1-piperazinyl)acetamides as pirenzepine models and some related compounds." Collection of Czechoslovak Chemical Communications 53, no. 8 (1988): 1820–44. http://dx.doi.org/10.1135/cccc19881820.

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Reactions of N-cyclohexyl-2-chloroacetamide, N-phenyl-2-chloroacetamide, N-(4-dimethylaminophenyl)-2-chloroacetamide, N-(2-nitrophenyl)-N-phenyl-2-chloroacetamide, its 3-nitrophenyl and 4-nitrophenyl analogues, N-(2-benzylphenyl)-2-chloroacetamide, 5-(chloroacetyl)-dibenz[b,f]azepine, and its 10,11-dihydro derivative with piperazine, 1-methylpiperazine, 2-(1-piperazinyl)ethanol, and 3-(1-piperazinyl)propanol resulted in compounds II, III, V-XV, XVIII, XXI, and XXIII, simple analogues of the antiulcer agent pirenzepine (I). Contributions to the syntheses and characterization of mianserin (XIX),

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37

Hu, Xiu-Rong, Jia-Li Ye, and Jian-Ming Gu. "Crystal structure of vilazodone hydrochloride methanol monosolvate." Acta Crystallographica Section E Crystallographic Communications 72, no. 12 (2016): 1783–85. http://dx.doi.org/10.1107/s2056989016017734.

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In the title compound, C26H28N5O2+·Cl−·CH3OH {systematic name: 4-(2-carbamoyl-1-benzofuran-5-yl)-1-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-ium chloride methanol monosolvate}, the protonated piperazine ring adopts a chair conformation. The indole ring plane is nearly perpendicular to the benzofuran ring system, with a dihedral angle of 85.77 (2)°. In the crystal, the organic cations, Cl−anions and methanol solvent molecules are linked by classical N—H...O and N—H...Cl hydrogen bonds, and weak C—H...O and C—H...π interactions into a three-dimensional supramolecular architecture.

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38

González Garcia, Filiberto, Eduardo M. Sampaio, Alessandra F. Neves, and Márcia G. de Oliveira. "Evaluación de la adherencia de uniones adhesivas metálicas con adhesivos epoxídicos modificados." Polímeros 18, no. 1 (2008): 30–44. http://dx.doi.org/10.1590/s0104-14282008000100009.

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En este trabajo fueron evaluadas las propiedades adhesivas de la resina epoxídica del tipo éter diglicidílico del bisfenol A. La resina fue modificada con dos modificadores poliméricos, uno de ellos un copolímero derivado del butadieno, y el otro un copolímero acrílico con el propósito de aumentar la tenacidad de la resina. Tres aminas alifáticas primarias fueron utilizadas como agentes de curado, trietilentetramina, N-(2-aminoetil)piperazina e isoforondiamina. Las propiedades adhesivas fueron investigadas usando la resina pura, así como la resina modificada. Las propiedades adhesivas de la re

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39

Šilhánková, Alexandra, Karel Šindelář, Karel Dobrovský, Ivan Krejčí, Jarmila Hodková, and Zdeněk Polívka. "Synthesis of New L-Proline Amides with Anticonvulsive Effect." Collection of Czechoslovak Chemical Communications 61, no. 7 (1996): 1085–92. http://dx.doi.org/10.1135/cccc19961085.

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Series of heterocyclic L-proline amides were prepared from BOC-L-proline and heterocyclic amines (mostly substituted piperazines and morpholines) via active ester with hydroxysuccinimide. 4-(4-Fluorobenzoyl)piperidine afforded L-proline 4-(4-(4-(4-fluorobenzoyl)piperidin-1-yl)benzoyl)piperidine (7b) simultaneously with expected L-proline 4-(4-fluorobenzoyl)piperidide (7a). D-Proline N-(3-(4-(3-chlorophenyl)piperazin-1-yl)propyl)amide (2) was prepared starting from D-proline. The amides were tested by methods of biochemical and behavioural pharmacology.

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40

Ullah, Nisar, and Helen Stoeckli-Evans. "Crystal structure and Hirshfeld surface analysis of the hydrochloride salt of 8-{4-[(6-phenylpyridin-3-yl)methyl]piperazin-1-yl}-3,4-dihydroquinolin-2(1H)-one." Acta Crystallographica Section E Crystallographic Communications 77, no. 2 (2021): 208–12. http://dx.doi.org/10.1107/s2056989021000979.

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The amine 8-{4-[(6-phenylpyridin-3-yl)methyl]piperazin-1-yl}-3,4-dihydroquinolin-2(1H)-one was crystallized as the hydrochloride salt, 4-(2-oxo-1,2,3,4-tetrahydroquinolin-8-yl)-1-[(6-phenylpyridin-3-yl)methyl]piperazin-1-ium chloride, C25H27N4 +·Cl− (I·HCl). The conformation of the organic cation is half-moon in shape enclosing the chloride anion. The piperidine ring of the 3,4-dihydroquinolin-2(1H)-one moiety has a screw-boat conformation, while the piperazine ring has a chair conformation. In the biaryl group, the pyridine ring is inclined to the phenyl ring by 40.17 (7) and by 36.86 (8)° to

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41

Little, Vanessa Renée, and Keith Vaughan. "Synthesis and characterization of a series of 1-methyl-4-[2-aryl-1-diazenyl]piperazines and a series of ethyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates." Canadian Journal of Chemistry 82, no. 8 (2004): 1294–303. http://dx.doi.org/10.1139/v04-081.

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1-Methylpiperazine was coupled with a series of diazonium salts to afford the 1-methyl-4-[2-aryl-1-diazenyl]piperazines (2), a new series of triazenes, which have been characterized by 1H and 13C NMR spectroscopy, IR spectroscopy, and elemental analysis. Assignment of the chemical shifts to specific protons and carbons in the piperazine ring was facilitated by comparison with the chemical shifts in the model compounds piperazine and 1-methylpiperazine and by a HETCOR experiment with the p-tolyl derivative (2i). A DEPT experiment with 1-methylpiperazine (6) was necessary to distinguish the meth

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42

Żesławska, Ewa, Wojciech Nitek, and Jadwiga Handzlik. "Conformational study of (Z)-5-(4-chlorobenzylidene)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-3H-imidazol-4(5H)-one in different environments: insight into the structural properties of bacterial efflux pump inhibitors." Acta Crystallographica Section C Structural Chemistry 73, no. 12 (2017): 1151–57. http://dx.doi.org/10.1107/s2053229617016461.

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The 2-amine derivatives of 5-arylidene-3H-imidazol-4(5H)-one are a new class of bacterial efflux pump inhibitors, the chemical compounds that are able to restore antibiotic efficacy against multidrug resistant bacteria. 5-Arylidene-3H-imidazol-4(5H)-ones with a piperazine ring at position 2 reverse the mechanisms of multidrug resistance (MDR) of the particularly dangerous Gram-negative bacteria E. coli by inhibition of the efflux pump AcrA/AcrB/TolC (a main multidrug resistance mechanism in Gram-negative bacteria, consisting of a membrane fusion protein, AcrA, a Resistant-Nodulation-Division p

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43

Abadleh, Mohammed M., Mustafa M. El-Abadelah, Salim S. Sabri, Hanan H. Mohammed, Malek A. Zihlif, and Wolfgang Voelter. "Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones." Zeitschrift für Naturforschung B 69, no. 7 (2014): 811–16. http://dx.doi.org/10.5560/znb.2014-4062.

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6aA set of new N2-(thien-3-yl)amidrazones (-h) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride 4(derived from 3-aminothiophene- 2-carboxylate) with the appropriate sec-cyclic amine. The antitumor activity of these compounds was evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines by a cell viability assay utilizing the tetrazolium dye (MTT). The amidrazone 6d encompassing the N-piperazine moiety, was the most active against MCF-7 and K562 with IC50 of 7.28 and 9:91 μM, respectively.

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44

Möhrle, Hans, and Katja Azodi. "Reaktionen Von Acetylencarbonsäureestern Mit Piperazinderivaten." Zeitschrift für Naturforschung B 61, no. 8 (2006): 1021–34. http://dx.doi.org/10.1515/znb-2006-0815.

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Hg(II)-EDTA-dehydrogenation of benzylpiperazine (5) in 50% ethanol with addition of diethyl acetylenedicarboxylate (2) to a minor extent gives rise to (piperazine-1,4-diyl)-bis(maleate) (9), which is inert to Hg(II)-EDTA and results in quantitative yield when Hg(II)-EDTA is omitted. 4- Benzylpiperazin-1-yl)-monomaleate (8) reacts with 2 in various solvents by addition of water with dealkylation and formation of 9. CH-acidic compounds may also be used as proton donors. Analogous reactions, although with minor yields, occur with the propiolates 11 and 12. 1-Substituted piperazines with benzyl, m

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45

Clifford, Sarah E., Vanny Tiwow, Aleasia Gendron, et al. "Complexation of Constrained Ligands Piperazine, N-substituted Piperazines, and Thiomorpholine." Australian Journal of Chemistry 62, no. 10 (2009): 1196. http://dx.doi.org/10.1071/ch09313.

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Complexation of the symmetric cyclic diamine piperazine (1,4-diazacyclohexane) has been examined in dry dimethyl formamide by spectrophotometric titrations (with Cu2+, Ni2+) to define formation constants, and by stopped-flow kinetics to define the complexation rates and reaction pathway. Initial formation of a rarely observed η1-piperazine intermediate occurs in a rapid second-order reactions. This intermediate then undergoes two competing reactions: formation of (chelated) η2-piperazine (ML) or the formation of (bridging) μ-piperazine (in M2L and M2L3, speciation depending on relative concent

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46

Żesławska, Ewa, Ewa Szymańska, Wojciech Nitek, and Jadwiga Handzlik. "Crystallographic studies of piperazine derivatives of 3-methyl-5-spirofluorenehydantoin in search of structural features of P-gp inhibitors." Acta Crystallographica Section C Structural Chemistry 77, no. 8 (2021): 467–78. http://dx.doi.org/10.1107/s2053229621006756.

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5-Spirofluorenehydantoin derivatives show efflux modulating, cytotoxic and antiproliferative effects in sensitive and resistant mouse T-lymphoma cells. In order to extend the knowledge available about the pharmacophoric features responsible for the glycoprotein P (P-gp) inhibitory properties of arylpiperazine derivatives of 3-methyl-5-spirofluorenehydantoin, we have performed crystal structure analyses for 1-[3-(3′-methyl-2′,4′-dioxospiro[fluorene-9,5′-imidazolidin]-1′-yl)propyl]-4-phenylpiperazine-1,4-diium dichloride monohydrate, C29H32N4O2 2+·2Cl−·H2O (1), 3′-methyl-1′-{3-[4-(4-nitrophenyl)

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47

Vejdělek, Zdeněk, and Miroslav Protiva. "N-(piperazinoacyl) and N-(piperazinoalkyl) derivatives of 4-cyclopentylaniline and related compounds: Synthesis and pharmacological screening." Collection of Czechoslovak Chemical Communications 51, no. 7 (1986): 1494–502. http://dx.doi.org/10.1135/cccc19861494.

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Five N-(4-cyclopentylphenyl)haloalkanecarboxamides were reacted with 1-methylpiperazine and 1-(2-hydroxyethyl)piperazine to give the corresponding N-(4-cyclopentylphenyl)piperazinoalkanecarboxamides Iab -Vab. Their reduction with lithium aluminium hydride afforded the triamines VIIab - XIab. Acylation of the N-(4-methylpiperazino)alkyl-4-cyclopentylanilines Xa and XIa with propionyl chloride resulted in the propionanilides XIVa and XVa, whereas a similar reaction of the N-(4-(2-hydroxyethyl)piperazino)alkyl-4-cyclopentylanilines VIIb and IXb - XIb produced the propionoxypropionanilides XIIc -

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48

Jílek, Jiří, Jiří Holubek, Emil Svátek, et al. "Potential metabolites of the neuroleptic agents belonging to the 8-methylthio-10-piperazino-10,11-dihydrodibenzo[b,f]thiepin series; Synthesis of 2-hydroxy and 3-hydroxy derivatives." Collection of Czechoslovak Chemical Communications 50, no. 10 (1985): 2179–90. http://dx.doi.org/10.1135/cccc19852179.

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The acid VI, prepared by reaction of potassium salts of (2-iodo-5-methoxyphenyl)acetic acid and 4-(methylthio)thiophenol in the presence of copper, was transformed via intermediates VII-IX to 2-methoxy-8-methylthio-10-piperazino-10,11-dihydrodibenzo[b,f]thiepins X and XI. Their demethylation with boron tribromide afforded 2-hydroxy derivatives of the neuroleptic agents methiothepin and oxyprothepin I and II. 11-Chloro-7-methoxy-2-methylthio-10,11-dihydrodibenzo[b,f]thiepin was subjected to substitution reactions with 1-methylpiperazine and 1-(ethoxycarbonyl)piperazine and gave piperazine deriv

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49

Harish Chinthal, Chayanna, Hemmige S. Yathirajan, Channappa N. Kavitha, Sabine Foro, and Christopher Glidewell. "The crystal structures of salts of N-(4-fluorophenyl)piperazine with four aromatic carboxylic acids and with picric acid." Acta Crystallographica Section E Crystallographic Communications 76, no. 8 (2020): 1179–86. http://dx.doi.org/10.1107/s2056989020008749.

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The structures are reported for five salts formed by reactions between N-(4-fluorophenyl)piperazine and aromatic acids. In 4-(4-fluorophenyl)piperazin-1-ium 2-fluorobenzoate monohydrate, C10H14FN2 +·C7H4FO2 −·H2O, (I), the components are linked by a combination of N—H...O and O—H...O hydrogen bonds to form a chain of alternating R 4 6(12) and R 6 6(16) rings. The ionic components of 4-(4-fluorophenyl)piperazin-1-ium 2-bromobenzoate 0.353-hydrate, C10H14FN2 +·C7H4BrO2 −·0.353H2O, (II), are linked by N—H...O hydrogen bonds to form a centrosymmetric four-ion aggregate containing an R 4 4(12) moti

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50

Abdel-Jalil, Raid J., Muhammad Saeed, Peter Heeg, and Wolfgang Voelter. "Synthesis and Properties of Selected 4-Substituted Anhydro Sugars." Zeitschrift für Naturforschung B 55, no. 7 (2000): 661–66. http://dx.doi.org/10.1515/znb-2000-0714.

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A new class of 4-deoxy-4-([4-substituted-1-piperazinyl], [4-morpholinyl] and [4-(perhydrol, 4-thiazin-4-yl)])-2,3-anhydrolyxopyranosides (3a-g and 6a-g) were synthesized from epoxy triflate moities 2 and 5 and 4-substituted piperazines, morpholines and perhydro-1,4- thiazines, respectively, to test their antibacterial activity. The characterized series of new compounds was tested in vitro against E. coli ATCC11229, S. aureus ATCC6538 and C. albicans SATCC10231.

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