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Synthesis and In-Silico Studies of Ortho-Fluorinated Benzenesulfonamides as Putative Anti-CETP Agents 作为拟抗 CETP 药物的正氟化苯磺酰胺的合成和室内研究
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-04-09 DOI: 10.2174/0113852728295939240315040152
Reema Abu Khalaf, Lama Jaradat, Maha Habash
: Cardiovascular disease is one of the primary causes of death. Atherosclerosis produces artery constriction or obstruction, which can lead to a heart attack or stroke. Cholesteryl Ester Transfer Protein (CETP) is a protein that aids in reverse cholesterol transport. It promotes cholesteryl ester transfer from HDL to LDL and VLDL. So, inhibition of CETP by drugs limits cardiovascular disease by decreasing LDL and increasing HDL cholesterol. In this study, ten ortho-fluoro substituted benzenesulfonamides 6a-6j were prepared, and their structure was fully determined using 1H NMR, 13C NMR, HR-MS, and IR. In vitro biological evaluation showed that compound 6d has the highest inhibitory activity with 100% inhibition, while compounds 6a-6c and 6e-6j had activities ranged from 29% - 83% at 10 μM concentration. Interestingly, para-substituted derivatives (6d, 6g, and 6j) were observed to have greater CETP inhibitory activities than their ortho- and meta- analogues irrespective to the nature of substituent, i.e., CH3, Cl, or NO2. Ligandfit docking experiment revealed the difference in the binding mode among the synthesized compounds, which is reflected in their CETP inhibitory activity. background: Cardiovascular disease is one of the primary causes of death. Atherosclerosis produces artery constriction or obstruction, which can lead to a heart attack or stroke. Cholesteryl ester transfer protein (CETP) is a protein that aids in reverse cholesterol transport. It promotes cholesteryl ester transfer from HDL to LDL and VLDL. So, inhibition of CETP by drugs limits cardiovascular disease by decreasing LDL and increasing HDL cholesterol. method: and their structure was fully determined using 1H-NMR, 13C-NMR, HR-MS, and IR. conclusion: Ligandfit docking experiment revealed the difference in the binding mode among the synthesized compounds which is reflected on their CETP inhibitory activity.
:心血管疾病是导致死亡的主要原因之一。动脉粥样硬化会造成动脉收缩或阻塞,从而导致心脏病发作或中风。胆固醇酯转移蛋白(CETP)是一种有助于胆固醇逆向运输的蛋白质。它能促进胆固醇酯从高密度脂蛋白转移到低密度脂蛋白和超低密度脂蛋白。因此,通过药物抑制 CETP 可以减少低密度脂蛋白,增加高密度脂蛋白胆固醇,从而限制心血管疾病的发生。本研究制备了 10 个正氟取代的苯磺酰胺类化合物 6a-6j,并使用 1H NMR、13C NMR、HR-MS 和 IR 全面测定了它们的结构。体外生物学评价结果表明,化合物 6d 的抑制活性最高,抑制率达 100%,而化合物 6a-6c 和 6e-6j 在 10 μM 浓度下的活性为 29% - 83%。有趣的是,对位取代衍生物(6d、6g 和 6j)的 CETP 抑制活性高于其正交和偏交类似物,而与取代基的性质(即 CH3、Cl 或 NO2)无关。Ligandfit docking 实验揭示了合成化合物在结合模式上的差异,这反映在它们的 CETP 抑制活性上:心血管疾病是导致死亡的主要原因之一。动脉粥样硬化会造成动脉收缩或阻塞,从而导致心脏病发作或中风。胆固醇酯转移蛋白(CETP)是一种有助于胆固醇逆向运输的蛋白质。它能促进胆固醇酯从高密度脂蛋白转移到低密度脂蛋白和超低密度脂蛋白。因此,通过药物抑制 CETP 可降低低密度脂蛋白胆固醇,增加高密度脂蛋白胆固醇,从而限制心血管疾病的发生。 方法:使用 1H-NMR、13C-NMR、HR-MS 和 IR 全面测定了它们的结构:Ligandfit docking 实验表明,合成的化合物之间的结合模式存在差异,这反映在它们对 CETP 的抑制活性上。
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引用次数: 0
Exploring Synthesis and Medicinal Applications of Andrographolide Derivatives: A Review 穿心莲内酯衍生物的合成与药物应用探索:综述
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-04-04 DOI: 10.2174/0113852728296785240308054135
Tanzeela Qadir, Shoaib Shaikh, Saadat A. Kanth, Jyotika Singh, Maria Baby, Praveen Kumar Sharma
: Andrographolide, derived from the plant Andrographis paniculata (AP), exhibits a diverse range of biological activities, encompassing anti-bacterial, anti-tumor, anti-inflammatory, anti-obesity, anti-viral, antifibrotic, hypoglycemic, and immunomodulatory properties. Notably, numerous analogs of andrographolide have been synthesized, incorporating significant chemical structural modifications to enhance bioavailability and druggability. A comprehensive exploration into their molecular and cellular mechanisms of action has also been undertaken, enriching our understanding. The investigation highlights the potential of related terpenoid analogs from Andrographis paniculata, beyond the diterpene lactone andrographolide, to hold promise in disease treatment due to structural similarities and diverse pharmacological effects. This review offers insights into the anticipated synthesis and therapeutic applications of andrographolide derivatives across a spectrum of disorders.
:穿心莲内酯提取自穿心莲(AP),具有多种生物活性,包括抗菌、抗肿瘤、抗炎、抗肥胖、抗病毒、抗纤维化、降血糖和免疫调节特性。值得注意的是,人们合成了许多穿心莲内酯类似物,对其化学结构进行了重大调整,以提高生物利用度和可药用性。此外,还对其分子和细胞作用机制进行了全面探索,丰富了我们的认识。这项研究强调了穿心莲中除二萜内酯穿心莲内酯以外的相关萜类类似物在疾病治疗方面的潜力,这些类似物具有结构相似性和不同的药理作用。本综述深入探讨了穿心莲内酯衍生物在各种疾病中的预期合成和治疗应用。
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引用次数: 0
Palladium-charcoal Catalyzed Direct Esterification of Aldehydes to Esters by NaIO4 钯炭催化 NaIO4 将醛直接酯化成酯
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-04-04 DOI: 10.2174/0113852728300082240308163721
Md. Mohinuddin, Kajol Ahmed, Izarul Islam, Anamul Hossain, Harendra N. Roy
:: An efficient direct oxidation method was developed to oxidize some aromatic and aliphatic aldehydes to esters by the dual utilization of NaIO4 and Pd-C. At ambient conditions, various aldehydes were employed in a clean esterification reaction to afford numerous esters in good to excellent yields. By this adopted method, some multifunctional aldehydes, high-energy-containing aromatic and unsaturated aldehydes, were advantageously oxidized to esters without noticeable difficulties. Moreover, no over-oxidation occurred to alcohols, and most byproducts were not formed during this oxidation process. Conventional and some modern methods lag behind owing to their easier operability and easy work-up process. This investigation has proven that the required oxidant (NaIO4) or catalyst (Pd-C) is useless to employ in excess, although some current methods utilize hugely expensive reagents for such conversions. Mundane reaction set-up, easy product recovery technique, non-toxic catalyst, and cheap and available starting materials are the noteworthy advantages of this method.
::研究人员开发了一种高效的直接氧化法,通过同时使用 NaIO4 和 Pd-C,将一些芳香族和脂肪族醛氧化成酯。在常温条件下,利用各种醛进行清洁的酯化反应,以良好至极佳的收率获得了多种酯。通过这种方法,一些多功能醛、高能量芳香族醛和不饱和醛被有效地氧化成酯,而不会出现明显的困难。此外,在此氧化过程中不会出现过度氧化成醇的情况,也不会产生大多数副产品。传统方法和一些现代方法之所以落后,是因为它们更易于操作,工作过程更简便。这项研究证明,过量使用所需的氧化剂(NaIO4)或催化剂(Pd-C)是没有用的,尽管目前的一些方法使用昂贵的试剂进行此类转化。这种方法的显著优点是:反应设置简单、产品回收技术容易、催化剂无毒、起始材料便宜易得。
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引用次数: 0
Synthesis of Aromatic Azides using Different Methodologies 使用不同方法合成芳香族叠氮化物
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-04-03 DOI: 10.2174/0113852728301737240307111549
Elisa Leyva, Silvia E. Loredo-Carrillo
:: For several decades, aromatic azides have been applied in diverse areas of research like synthesis of organic compounds, novel materials and photoaffinity labeling of biomolecules. The discovery of click chemistry and bioorthogonal chemistry expanded their applications. Currently, they are extensively used in biology, biochemistry and medicine. For many years, aromatic azides were usually prepared using nucleophilic substitution. In this classical procedure, commercially available anilines are first converted into aryl diazonium salts which in turn are transformed into aromatic azides by nucleophilic substitution with sodium azide. However, this procedure is rather inconvenient experimentally since it requires the use of strong acids and low temperatures. In recent years, several alternative procedures have been developed. In the present review, we present the synthesis of aromatic azides by means of different experimental methodologies.
::几十年来,芳香叠氮化物一直被应用于有机化合物的合成、新型材料和生物大分子的光亲和标记等多个研究领域。点击化学和生物正交化学的发现扩大了它们的应用范围。目前,它们被广泛应用于生物学、生物化学和医学领域。多年来,芳香叠氮化物通常采用亲核取代法制备。在这一经典程序中,市售苯胺首先被转化为芳基重氮盐,然后通过与叠氮化钠的亲核取代作用转化为芳香叠氮化物。然而,这一过程需要使用强酸和低温,因此在实验上非常不便。近年来,人们开发出了几种替代程序。在本综述中,我们介绍了通过不同实验方法合成芳香叠氮化物的过程。
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引用次数: 0
A Review on the Development of Polymer Supported Heterogeneous Palladium Materials for Organic Synthesis and Electrochemical Applications 聚合物支撑的异质钯材料在有机合成和电化学应用中的发展综述
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-04-02 DOI: 10.2174/0113852728299173240302041524
Ashlesha P. Kawale, Nishant Shekhar, Arti Srivastava, Subhash Banerjee
:: This comprehensive review explores the advancements in catalytic transformation, focusing on the use of heterogeneous catalytic systems with a particular emphasis on polymeric-supported palladium (Pd) complexes. This study explores the limitations associated with conventional homogeneous reagents, emphasizes the transition to eco-friendly catalytic systems, and emphasizes the importance of Pd nanoparticles. These nanoparticles are particularly noteworthy for their distinctive properties, including elevated catalytic activity, making them promising for various applications in organic synthesis. The review thoroughly examines the design and synthesis of heterogeneous catalysts, emphasizing the crucial selection of safe and recyclable supports to augment the longevity and reusability of metallic catalysts. Diverse polymer varieties, including polystyrene (PS), polyethylene (PE), polyacrylate derivatives, polyethylene glycol (PEG), and grafted polymers, are investigated as viable supports for Pd complexes. The authors intricately describe the synthesis techniques for these polymer-supported Pd catalysts and furnish illustrative examples showcasing their effectiveness in organic transformation. This comprehensive review additionally highlights the synthesis of polymer-supported palladium (Pd) materials and discusses their applications in electrochemistry. The focus extends to the electrocatalytic properties of Pdbased polymeric nanomaterials, showcasing their effectiveness in glucose sensing, hydrogen peroxide detection, and the sensing of other biological analytes. Furthermore, the catalytic capabilities of Pd nanoparticles in various electrochemical applications, including wastewater treatment and electrochemical capacitors, are explored. Integrating polymer-supported Pd materials into these electrochemical processes underscores their versatility and potential contributions to advancements in catalysis and electrochemical sensing. Catalytic applications featuring polymer-supported palladium complexes with polymeric ligands in organic synthesis processes use the Sonogashira reaction, Suzuki-Miyaura coupling, Heck reaction, Catalytic asymmetric transformations, etc. The subsequent section of the paper focuses on the creation of polymeric palladium complexes, achieved by the complexation of polymeric ligands with palladium precursors. It delves into noteworthy examples of catalytic processes employing polymer-supported palladium complexes featuring polymeric ligands, emphasizing distinct polymers, such as PS, PE, polyacrylate derivatives, PEG, and grafting polymers. The review concludes by exploring catalytic asymmetric transformations using chiral palladium complexes immobilized on polymer supports and discusses various chiral ligands and their immobilization on polymer supports, emphasizing their application in asymmetric allylic alkylation. The review furnishes a comprehensive summary of recent advancements, challenges, and prospective avenues in
::这篇综合综述探讨了催化转化方面的进展,重点是异质催化体系的使用,特别强调聚合物支撑的钯(Pd)络合物。本研究探讨了传统均相试剂的局限性,强调了向生态友好型催化体系的过渡,并强调了钯纳米颗粒的重要性。这些纳米颗粒因其独特的性质(包括较高的催化活性)而特别值得关注,使其在有机合成的各种应用中大有可为。该综述深入探讨了异相催化剂的设计与合成,强调了选择安全、可回收的载体以延长金属催化剂的寿命并提高其重复利用率的重要性。研究了各种聚合物,包括聚苯乙烯 (PS)、聚乙烯 (PE)、聚丙烯酸酯衍生物、聚乙二醇 (PEG) 和接枝聚合物,作为钯复合物的可行支撑物。作者详细描述了这些聚合物支撑钯催化剂的合成技术,并举例说明了它们在有机转化中的有效性。本综述还重点介绍了聚合物支撑的钯(Pd)材料的合成,并讨论了它们在电化学中的应用。重点延伸到钯基聚合物纳米材料的电催化特性,展示了它们在葡萄糖传感、过氧化氢检测和其他生物分析物传感中的有效性。此外,还探讨了钯纳米粒子在废水处理和电化学电容器等各种电化学应用中的催化能力。将聚合物支撑的钯材料整合到这些电化学过程中,凸显了它们的多功能性以及对催化和电化学传感领域进步的潜在贡献。在有机合成过程中,聚合物支持的钯配合物与聚合物配体的催化应用包括:Sonogashira 反应、Suzuki-Miyaura 偶联、Heck 反应、催化不对称转化等。论文接下来的部分重点介绍了通过聚合物配体与钯前体的络合反应生成聚合物钯络合物的过程。论文深入探讨了采用聚合物配体的聚合物支撑钯络合物的催化过程中值得注意的实例,重点介绍了不同的聚合物,如 PS、PE、聚丙烯酸酯衍生物、PEG 和接枝聚合物。综述最后探讨了固定在聚合物载体上的手性钯配合物的催化不对称转化,并讨论了各种手性配体及其在聚合物载体上的固定,强调了它们在不对称烯丙基烷基化中的应用。综述全面总结了聚合物载体钯催化剂在电化学应用催化氧化方面的最新进展、挑战和前景。
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引用次数: 0
Synthesis, Characterization, Antimicrobial Activity, and Molecular Docking Study of Newer Chalcone-based Triazolo Pyrimidine Compounds 新型查耳酮基三唑并嘧啶化合物的合成、表征、抗菌活性和分子对接研究
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-04-02 DOI: 10.2174/0113852728298472240305110906
Monik Gohil, Siva Prasad Das, Jeena Jyoti Boruah
:: In this work, we present the synthesis of a newer series of 15 chalcone-based pyrimidine compounds 4a-o. All the compounds were characterized by elemental analysis, melting point determination, mass, FTIR, and NMR analysis. We have evaluated the antimicrobial activity of these compounds. The compounds showed good inhibition activity towards different bacterial and fungal species such as S. aureus, S. pneumonia, E. coli, P. aeruginosa, Candida albicans, Aspergillus niger, and Alternaria alternata. Compounds 4c, 4h, 4k, and 4g showed comparable activities to those of commercially available drugs. Molecular docking study showed good interaction between each of the compounds and DNA gyrase enzyme. The docking score of the compounds ranges between -8.0 to -8.9 kcal/mol. Further, the ADMET analysis indicated the potential of the compounds as a drug candidate.
::在这项工作中,我们合成了一系列较新的 15 个基于查耳酮的嘧啶化合物 4a-o。我们通过元素分析、熔点测定、质量、傅立叶变换红外光谱和核磁共振分析对所有化合物进行了表征。我们评估了这些化合物的抗菌活性。这些化合物对金黄色葡萄球菌、肺炎双球菌、大肠杆菌、绿脓杆菌、白色念珠菌、黑曲霉和交替孢霉等不同细菌和真菌表现出良好的抑制活性。化合物 4c、4h、4k 和 4g 显示出与市售药物相当的活性。分子对接研究表明,每种化合物与 DNA 回旋酶之间都有良好的相互作用。化合物的对接得分在 -8.0 至 -8.9 kcal/mol 之间。此外,ADMET 分析表明这些化合物具有候选药物的潜力。
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引用次数: 0
Chirality Sensing in Coordination-driven Supramolecular Assemblies 配位驱动超分子组装中的手性传感
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-28 DOI: 10.2174/0113852728292501240301062823
Abhik Paul, Subhadip Roy
: Chirality is a widespread structural characteristic found in nature and plays a vital role in the structure and functioning of almost all biological systems. Nevertheless, the translation of chirality into synthetic systems is highly intricate yet captivating, as it not only applies fundamental understanding but also has the potential to tackle significant difficulties in biochemistry and medicine. Structurally, the process of coordination- driven self-assembly involves the organization of basic molecular components into well-defined porous homochiral metal-organic cages (MOCs). This allows for a systematic investigation of the enantioselective processes occurring within the nanocavities, which have limited space and specific chiral microenvironments. This article aims to provide a comprehensive summary of the recent advancements in supramolecular chirality generated in the fascinating class of porous MOCs. It will cover the synthesis and characterization of these materials, as well as the implications of their stereochemical information in terms of chiral recognition and enantio- separation. Subsequently, a subjective viewpoint will be presented regarding the potential, possibilities, and significant challenges in the future advancement of this domain, aiming to expand the progress in creating novel chiral functional materials in the realm of chemistry and beyond.
:手性是自然界中广泛存在的一种结构特征,在几乎所有生物系统的结构和功能中都发挥着至关重要的作用。然而,将手性转化为合成系统的过程非常复杂,但却非常吸引人,因为它不仅应用了基本的理解,而且有可能解决生物化学和医学中的重大难题。从结构上讲,配位驱动自组装过程涉及将基本分子成分组织成定义明确的多孔同手性金属有机笼(MOCs)。这样就可以对纳米空腔内发生的对映选择性过程进行系统研究,因为纳米空腔的空间有限,而且存在特定的手性微环境。本文旨在全面总结多孔 MOCs 这一迷人类别中产生的超分子手性的最新进展。文章将介绍这些材料的合成和表征,以及其立体化学信息在手性识别和对映体分离方面的影响。随后,将就这一领域未来发展的潜力、可能性和重大挑战提出主观观点,旨在扩大在化学及其他领域创造新型手性功能材料的进展。
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引用次数: 0
Multicomponent 3D-printed Collagen-based Scaffolds for Cartilage Regeneration: Recent Progress, Developments, and Emerging Technologies 用于软骨再生的多组分三维打印胶原基支架:最新进展、发展和新兴技术
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-25 DOI: 10.2174/0113852728293437240227065230
Babak Mikaeeli Kangarshahi, Seyed Morteza Naghib
: Cartilage tissue presents challenges in terms of repair and regeneration due to its inherent limitations in self-healing and the scarcity of available donors. Cartilage damage can result in the development of joint problems characterized by symptoms, such as pain, swelling, and osteoarthritis. Collagen scaffolds are extensively used as biomimetic substances for cartilage engineering due to their ability to offer structural, biochemical, and mechanical signals for chondrocytes. Nevertheless, traditional techniques for producing collagen scaffolds frequently yield inadequate pore architecture, diminished mechanical robustness, and restricted form accuracy. Hence, 3D printing is a developing method that can surpass these restrictions by allowing accurate manipulation of the shape, porousness, and makeup of the scaffold. 3D printing has the capability to include various materials and cells in the scaffolds, resulting in the production of intricate and personalized tissue structures. This research examines the latest progress in utilizing 3D printing to create collagen scaffolds for the purpose of regenerating cartilage. This text discusses the different sources of collagen, methods of cross-linking, techniques for printing, and strategies for post-processing that are employed to improve the performance of scaffolds. Furthermore, it discusses the difficulties and potential future paths of utilizing 3D printing to create collagen scaffolds for the purpose of regenerating cartilage.
:软骨组织在自我修复方面存在固有的局限性,而且可用的供体稀缺,因此在修复和再生方面面临挑战。软骨损伤会导致以疼痛、肿胀和骨关节炎等症状为特征的关节问题。胶原支架可为软骨细胞提供结构、生化和机械信号,因此被广泛用作软骨工程的生物仿生物质。然而,生产胶原支架的传统技术经常会产生孔隙结构不足、机械坚固性降低和形状精度受限等问题。因此,三维打印是一种新开发的方法,它可以精确地操纵支架的形状、孔隙度和构成,从而超越这些限制。三维打印能够在支架中加入各种材料和细胞,从而制造出复杂的个性化组织结构。本研究探讨了利用三维打印技术制造胶原支架用于软骨再生的最新进展。本文讨论了胶原蛋白的不同来源、交联方法、打印技术以及为提高支架性能而采用的后处理策略。此外,它还讨论了利用三维打印技术制造胶原支架用于软骨再生的困难和未来可能的发展方向。
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引用次数: 0
Synthesis of Polypeptides by Ring-opening Polymerization: A Concise Review 开环聚合法合成多肽:简明综述
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-25 DOI: 10.2174/0113852728274519240228105518
Mostafa Badreldin, Pedro Salas-Ambrosio, Marcela Ayala, Simon Harrisson, Colin Bonduelle
: The most economical and efficient route to prepare polypeptides from synthetic chemistry is through the Ring-Opening Polymerization (ROP) of amino acids using N-carboxyanhydride (NCA) monomers. Peptide polymers, in contrast to proteins, consist of repeated amino acid units and are comparatively simpler macromolecules. Despite their simplicity, these polypeptides offer a unique combination of beneficial traits found in both synthetic polymers (such as solubility, processability, and rubber elasticity) and natural proteins (including secondary structure, functionality, and biocompatibility). Nevertheless, NCA polymerization faces significant challenges, including intricate monomer purification and the necessity for processing toxic solvents. In this context, this review presents the fundamental principles of this polymer chemistry, the synthesis of NCA monomers, and the different methodologies to access polypeptides by ROP. It also explores the most recent advances in this field of research, with a focus on how new methods enable the use of more reactive initiators and the development of original processes, including the use of aqueous solvents.
:通过化学合成制备多肽最经济、最有效的方法是使用 N-羧基酸酐(NCA)单体对氨基酸进行开环聚合(ROP)。与蛋白质相比,多肽聚合物由重复的氨基酸单元组成,是一种相对简单的大分子。尽管这些多肽非常简单,但却能将合成聚合物(如溶解性、加工性和橡胶弹性)和天然蛋白质(包括二级结构、功能性和生物相容性)中的有益特性独特地结合在一起。然而,NCA 聚合面临着巨大的挑战,包括复杂的单体纯化和加工有毒溶剂的必要性。在此背景下,本综述介绍了这种聚合物化学的基本原理、NCA 单体的合成以及通过 ROP 获取多肽的不同方法。它还探讨了这一研究领域的最新进展,重点是新方法如何使人们能够使用更具反应性的引发剂和开发原始工艺,包括使用水性溶剂。
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引用次数: 0
Cobalt (III)–porphyrin Complex as an Efficient and Recyclable Homogeneous Catalyst for the Synthesis of Tetrahydro-2-oxa-4-thia-diazapentalen-5-one Derivatives in Aqueous Medium 在水介质中合成四氢-2-氧杂-4-硫杂氮杂环戊烯-5-酮衍生物的高效可循环均相催化剂钴 (III)-卟啉配合物
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-19 DOI: 10.2174/0113852728295698240220081550
Hany M. Abd El-Lateef, Thomas Nady A. Eskander, Mohammad Saleh Hussein Alzubi, Mai M. Khalaf, Mahmoud Abd El Aleem Ali El-Remaily
: In this study, we successfully synthesized the CoPHrn complex as an efficient and recyclable catalyst for the one-pot, three-component reaction of aromatic aldehydes, 2,4-thiazolidenedione, and hydroxylamine hydrochloride, leading to the synthesis of tetrahydro-2-oxa-4-thia-diazapentalen-5-one derivatives under environmentally friendly conditions. The structures of the newly formed compounds were determined through elemental and spectral analyses. This methodology offers significant advantages, including its eco-friendliness, cost-effectiveness, operational simplicity, extensive reusability, and applicability, as well as the easy recovery of the catalyst using straightforward methods. Additionally, a series of tetrahydro-2-oxa-4-thia-diazapentalen-5- one derivatives were successfully synthesized. Notably, this novel procedure demonstrates remarkable benefits in terms of safety, simplicity, stability, mild reaction conditions, short reaction times, excellent yields, and high purity, all achieved without the use of hazardous solvents.
在这项研究中,我们成功合成了 CoPHrn 复合物,它是一种高效且可回收的催化剂,可用于芳香醛、2,4-噻唑烷二酮和盐酸羟胺的一锅三组分反应,从而在环境友好的条件下合成四氢-2-氧杂-4-噻二氮杂戊烯-5-酮衍生物。通过元素分析和光谱分析确定了新生成化合物的结构。该方法具有环保、成本效益高、操作简单、重复利用率高和适用性强等显著优势,而且催化剂易于通过简单的方法回收。此外,还成功合成了一系列四氢-2-氧杂-4-硫杂-5-氮杂戊烯衍生物。值得注意的是,这种新型方法在安全、简单、稳定、反应条件温和、反应时间短、产率高和纯度高等方面都有显著优势,而且无需使用有害溶剂。
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引用次数: 0
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Current Organic Chemistry
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