scholarly journals Synthesis, Characterization and Biological Activate 5-(Hydroxymethyl) Pyrrolidin-2-One at Room Temperature

Author(s):  
Veerappan Jeyachandran

<p>A new class of chiral pyrrolidinone was synthesized from (5S)-5-[(trityloxy)methyl] pyrrolidin-2-one (6) (Schemes 1 and 2). The synthetic design followed led to the insertion of various substituents at 1 and 5 of the pyrrolidinone moiety. Some of them possess two or three stereo centers, here configuration was retained under the mild condition. The new compounds also carry an imidazole moiety, which, along with the 2-pyrrolidinone template, may prove pivotal to several biological processes. The chiral pyrrolidinone (R) ring is incorporatedin various compounds with biological and pharmaceutical activities [1]. some of them are well known medicines, e.g., doxapram for patients with respiratory failure,piracetam for patients with Alzheimer’s seizures, and senile dementia, concussion and other neurological problems [2,3]. The properties and applications of pyroglutamic acid as a versatile building block in asymmetric synthesis has extensively been reviewed in the literature[4,5]. Some of them exhibited anti-inflammatory and antihypertensive activity [6,7]</p>

1969 ◽  
Vol 47 (2) ◽  
pp. 339-342 ◽  
Author(s):  
L. K. Peterson ◽  
K. I. Thé

Reactions between organo-arsine derivatives (CF3)2AsX and (CF3)3As and hydrazine or substituted hydrazines are discussed as synthetic routes to a new class of hydrazinoarsine compounds. The systems [(CF3)2As]x N2H4−x are unstable with respect to elimination of CF3H and N2, but stability increases with increased methylation of the nitrogen atoms. The new compounds described are: N-methyl, N′-bis(trifluoromethyl)arsinohydrazine, MeNHNHAs(CF3)2, (1) (highly unstable at room temperature); N,N-dimethyl, N′-bis(trifluoromethyl)arsinohydrazine, Me2NNHAs(CF3)2, (2) (m.p. 3.00° ± 0.15°, b.p. 20°/14.6 mm); and trimethylhydrazino-bis(trifluoromethyl)arsine, Me2NNMeAs(CF3)2, (3) (m.p. −41.5° ± 0.5°, b.p. 15°/6.30 mm). The observed order of stability was [Formula: see text]


2000 ◽  
Vol 626 ◽  
Author(s):  
Duck-Young Chung ◽  
Melissa A. Lane ◽  
John R. Ireland ◽  
Paul W. Brazis ◽  
Carl R. Kannewurf ◽  
...  

ABSTRACTBased on the versatile combination of PbQ- and Bi2Q3-type (Q = S, Se, Te) fragments, we explored new compounds in the Pb/Bi/Se ternary system. The new class of compounds, Pb5Bi6Se14, Pb5Pb12Se23, and PbBi8Se13 are homologues with different combination of alternating Bi2Se3- and PbSe-type layers. α- and β-Pb6Bi2Se9 were obtained in different synthetic conditions and the former is isostructural to heyrovskyite (Pb6Bi2S9) while the latter is a NaCl-type cubic phase. Pb5Bi6Se14 shows a power factor of 11.2 μW/cm·K2 with electrical conductivity of 657 S/cm and thermopower of -131 μV/K at 271 K. The most significant characteristic of this material is the extremely low thermal conductivity of less than 1.0 W/m·K at room temperature. On the basis of these properties, a preliminary doping study for Pb5Bi6Se14 with Sn, Sb, and SbBr3 as dopants was undertaken and the results are presented in this report.


Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 81
Author(s):  
Anna Carbone ◽  
Stella Cascioferro ◽  
Barbara Parrino ◽  
Daniela Carbone ◽  
Camilla Pecoraro ◽  
...  

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 µM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents.


2017 ◽  
Vol 38 (1) ◽  
pp. 97-110 ◽  
Author(s):  
Artur Kubiczek ◽  
Władysław Kamiński

AbstractRoom-temperature ionic liquids (RTILs) are a moderately new class of liquid substances that are characterized by a great variety of possible anion-cation combinations giving each of them different properties. For this reason, they have been termed as designer solvents and, as such, they are particularly promising for liquid-liquid extraction, which has been quite intensely studied over the last decade. This paper concentrates on the recent liquid-liquid extraction studies involving ionic liquids, yet focusing strictly on the separation of n-butanol from model aqueous solutions. Such research is undertaken mainly with the intention of facilitating biological butanol production, which is usually carried out through the ABE fermentation process. So far, various sorts of RTILs have been tested for this purpose while mostly ternary liquid-liquid systems have been investigated. The industrial design of liquid-liquid extraction requires prior knowledge of the state of thermodynamic equilibrium and its relation to the process parameters. Such knowledge can be obtained by performing a series of extraction experiments and employing a certain mathematical model to approximate the equilibrium. There are at least a few models available but this paper concentrates primarily on the NRTL equation, which has proven to be one of the most accurate tools for correlating experimental equilibrium data. Thus, all the presented studies have been selected based on the accepted modeling method. The reader is also shown how the NRTL equation can be used to model liquid-liquid systems containing more than three components as it has been the authors’ recent area of expertise.


Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2662
Author(s):  
Nathalie Audebrand ◽  
Antoine Demont ◽  
Racha El Osta ◽  
Yuri V. Mironov ◽  
Nikolay G. Naumov ◽  
...  

The reaction of the K4[{Re6Si8}(OH)a6]·8H2O rhenium cluster salt with pyrazine (Pz) in aqueous solutions of alkaline or alkaline earth salts at 4 °C or at room temperature leads to apical ligand exchange and to the formation of five new compounds: [trans-{Re6Si8}(Pz)a2(OH)a2(H2O)a2] (1), [cis-{Re6Si8}(Pz)a2(OH)a2(H2O)a2] (2), (NO3)[cis-{Re6Si8}(Pz)a2(OH)a(H2O)a3](Pz)·3H2O (3), [Mg(H2O)6]0.5[cis-{Re6Si8}(Pz)a2(OH)a3(H2O)a]·8.5H2O (4), and K[cis-{Re6Si8}(Pz)a2(OH)a3(H2O)a]·8H2O (5). Their crystal structures are built up from trans- or cis-[{Re6Si8}(Pz)a2(OH)a4−x(H2O)ax]x−2 cluster units. The cohesions of the 3D supramolecular frameworks are based on stacking and H bonding, as well as on H3O2−bridges in the cases of (1), (2), (4), and (5) compounds, while (3) is built from stacking and H bonding only. This evidences that the nature of the synthons governing the cluster unit assembly is dependent on the hydration rate of the unit.


Synthesis ◽  
2022 ◽  
Author(s):  
Dishu Zeng ◽  
Tianbao Yang ◽  
Niu Tang ◽  
Wei Deng ◽  
Jiannan Xiang ◽  
...  

A simple, mild, green and efficient method for the synthesis of 2-aminobenzamides was highly desired in organic synthesis. Herein, we developed an efficient, one-pot strategy for the synthesis of 2-aminobenzamides with high yields irradiated by UV light. 32 examples proceeded successfully by this photo-induced protocol. The yield reached up to 92%. The gram scale was also achieved easily. This building block could be applied in the preparation of quinazolinones derivatives. Amino acid derivatives could be employed smoothly at room temperature. Finally, a plausible mechanism was proposed.


2021 ◽  
Author(s):  
Quan-Xi Shi ◽  
Qian Li ◽  
Hang Xiao ◽  
Xiaoli Sun ◽  
Hongli Bao ◽  
...  

Carboxylic acids are widely available from both biomass and fossil sources on the earth. In comparison with multifunctional carboxylic acid containing chemicals those have been comprehensively used as building block...


2017 ◽  
Vol 69 (9) ◽  
pp. 2319-2331 ◽  
Author(s):  
Muhammad Jamil ◽  
Boubacar A Kountche ◽  
Imran Haider ◽  
Xiujie Guo ◽  
Valentine O Ntui ◽  
...  

abstract Strigolactones (SLs) are a new class of phytohormones that also act as germination stimulants for root parasitic plants, such as Striga spp., and as branching factors for symbiotic arbuscular mycorrhizal fungi. Sources for natural SLs are very limited. Hence, efficient and simple SL analogs are needed for elucidating SL-related biological processes as well as for agricultural applications. Based on the structure of the non-canonical SL methyl carlactonoate, we developed a new, easy to synthesize series of analogs, termed methyl phenlactonoates (MPs), evaluated their efficacy in exerting different SL functions, and determined their affinity for SL receptors from rice and Striga hermonthica. Most of the MPs showed considerable activity in regulating plant architecture, triggering leaf senescence, and inducing parasitic seed germination. Moreover, some MPs outperformed GR24, a widely used SL analog with a complex structure, in exerting particular SL functions, such as modulating Arabidopsis roots architecture and inhibiting rice tillering. Thus, MPs will help in elucidating the functions of SLs and are promising candidates for agricultural applications. Moreover, MPs demonstrate that slight structural modifications clearly impact the efficiency in exerting particular SL functions, indicating that structural diversity of natural SLs may mirror a functional specificity.


2015 ◽  
Vol 51 (43) ◽  
pp. 8939-8941 ◽  
Author(s):  
Sandra Medina ◽  
Alexander S. Henderson ◽  
John F. Bower ◽  
M. Carmen Galan

The use of (salen)Co catalysts as a new class of bench-stable stereoselective glycosylation promoters of trichloroacetimidate glycosyl donors at room temperature is described.


2021 ◽  
Vol 14 (11) ◽  
pp. 1125
Author(s):  
Everton M. da Silva ◽  
Hérika D. A. Vidal ◽  
Arlene G. Corrêa

Viral infections cause many severe human diseases, being responsible for remarkably high mortality rates. In this sense, both the academy and the pharmaceutical industry are continuously searching for new compounds with antiviral activity, and in addition, face the challenge of developing greener and more efficient methods to synthesize these compounds. This becomes even more important with drugs possessing stereogenic centers as highly enantioselective processes are required. In this minireview, the advances achieved to improve synthetic routes efficiency and sustainability of important commercially antiviral chiral drugs are discussed, highlighting the use of organocatalytic methods.


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