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Application of Hydroxy Propargylic Alcohols in Organic Synthesis. 羟基丙炔醇在有机合成中的应用。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-29 DOI: 10.1002/tcr.202500266
S Pravinkumar, Attunuri Nagireddy, Hamesh Basumatary, Adita S Madavi, Prathap Reddy Mukthapuram, Rajesh Manda

Propargylic alcohol is a shining star in the chemical space. These congeners have garnered significant attention from the synthetic chemistry community due to their dual functionality and three-centered reactivity. In this realm, the electrophilic cyclization of propargylic alcohols with a tethered nucleophile functional group is a key strategy for synthesizing hetero- and carbocycles. In these transformations, the position of the nucleophilic reactive handle can influence the reaction outcome. Consequently, these derivatives open up numerous opportunities to create complex cyclic adducts through various reaction pathways. Among all nucleophile tethers, the hydroxy group has been increasingly used in the production of oxy-heterocyclics. The hydroxy dialing on the core propargylic alcohol would lead to oxy-heterocyclics, such as benzofuran, furan, chromene, coumarin, chromone, pyrane, etc., which have numerous applications in various fields of biology and other scientific fields. In this review, we focused on uncovered hydroxy-tethered propargylic alcohol cyclization reactions. We categorized these transformations based on the structural features of hydroxy propargylic alcohols. With this review, we aim to pave the way for further efforts in discovering new reaction pathways.

丙炔醇是化学领域中一颗闪亮的明星。这些同源物由于其双重功能和三中心反应性而引起了合成化学界的极大关注。在这个领域中,带亲核官能团的丙炔醇的亲电环化是合成杂环和碳环的关键策略。在这些转化中,亲核反应柄的位置会影响反应的结果。因此,这些衍生物开辟了许多机会,以创造复杂的环加合物通过各种反应途径。在所有亲核系链中,羟基已越来越多地用于生产含氧杂环。丙炔醇核心上的羟基拨号会生成氧杂环,如苯并呋喃、呋喃、铬、香豆素、铬酮、吡喃等,这些化合物在生物学和其他科学领域有着广泛的应用。在这篇综述中,我们主要关注未发现的羟基系链丙炔醇环化反应。我们根据羟基丙炔醇的结构特征对这些转化进行了分类。通过这一综述,我们的目标是为进一步发现新的反应途径铺平道路。
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引用次数: 0
Front Cover: Advancements in the Design and Development of Organic Fluorophores for the Excited State Intramolecular Proton Transfer Phenomenon (Chem. Rec. 11/2025) 封面:用于激发态分子内质子转移现象的有机荧光团的设计与开发进展(化学)。Rec。11/2025)
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-27 DOI: 10.1002/tcr.70062
Gargi Mishra, Durgesh Singh, Surabhi Asthana, Himanshu Shekhar Tripathi, Rampal Pandey, Mrituanjay D. Pandey

Excited-state intramolecular proton transfer (ESIPT) happens when a molecule, upon photon absorption, is promoted to an electronically excited state, where a proton transfer occurs from a donor to an acceptor group within the molecule. This process generates an excited-state tautomer, often exhibiting a lower ionization potential. Consequently, the fluore scence spectra display a notable Stokes shift, with emission peaks shifted toward longer wavelengths. More details can be found in the Review by Rampal Pandey, Mrituanjay D. Pandey, and co-workers (DOI: 10.1002/tcr.202500109).

激发态分子内质子转移(ESIPT)发生在光子吸收后,分子被提升到电子激发态,其中质子从分子内的供体基团转移到受体基团。这个过程产生激发态互变异构体,通常表现出较低的电离电位。因此,荧光光谱显示出明显的斯托克斯位移,发射峰向更长的波长移动。更多细节可以在Rampal Pandey, Mrituanjay D. Pandey及其同事的评论中找到(DOI: 10.1002/tcr.202500109)。
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引用次数: 0
Thiazolotriazoles: Their Biological Activity and Structure-Activity Relationships. 噻唑三唑类化合物的生物活性及其构效关系。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-27 DOI: 10.1002/tcr.202500151
Umadevi Kizhakke Purakkel, Ganji Praveena, Ewan W Blanch, Subashani Maniam

Thiazolotriazole is gaining attention in medicinal chemistry due to its wide spectrum of biological activity. It is a fused heterocyclic compound formed by the fusion of 1,3-thiazole and 1,2,4-triazole, and the type of ring fusion results in the formation of isomeric thiazolotriazoles-[3,2-b] or [2,3-c] isomers. The synthesis of both ring systems has been carried out by various methodologies ranging from conventional methods such as cyclization and annulation to the use of metal catalysts, microwave radiation, photochemical and multicomponent reactions. In drug discovery, thiazolotriazole derivatives have been primarily investigated for their antibacterial, anticancer, anti-inflammatory, and antifungal properties. Recent years have seen significant advancements in anticancer drug research, revealing that these molecules are potential anticancer agents interacting with specific targets or biochemical pathways responsible for apoptosis and proliferation. In addition, thiazolotriazole also exhibits analgesic, anticonvulsant, antidiabetic, and antioxidant activities. Furthermore, thiazolotriazoles have also demonstrated the potential to inhibit enzymes such as carbonic anhydrase, urease, cyclooxygenase, and butyrylcholinesterase, which are meant to have particular biological functions. In the context of various applications, a review that describes biological activities with a particular focus on structural attributes that contribute to the activity will be helpful to better understand structure-activity relationship (SAR) and guide for further design of bioactive thiazolotriazoles. This review explains the biological activity of thiazolotriazole highlighting SAR and drug targets for specific disease conditions which will be helpful to better understand the scaffold and apply this knowledge to future drug discovery on thiazolotriazoles.

噻唑三唑具有广泛的生物活性,在药物化学领域受到越来越多的关注。它是一种由1,3-噻唑和1,2,4-三唑融合形成的融合杂环化合物,这种环融合的类型导致形成异构体噻唑三唑-[3,2-b]或[2,3-c]异构体。这两种环系的合成已通过各种方法进行,从传统的环化和环化方法到使用金属催化剂、微波辐射、光化学和多组分反应。在药物发现方面,噻唑三唑衍生物主要因其抗菌、抗癌、抗炎和抗真菌的特性而被研究。近年来,抗癌药物研究取得了重大进展,表明这些分子是潜在的抗癌药物,与负责细胞凋亡和增殖的特定靶点或生化途径相互作用。此外,噻唑三唑还具有镇痛、抗惊厥、抗糖尿病和抗氧化活性。此外,噻唑三唑也被证明具有抑制酶的潜力,如碳酸酐酶、脲酶、环加氧酶和丁基胆碱酯酶,这些酶具有特殊的生物学功能。在各种应用的背景下,对生物活性进行综述,特别关注对活性有贡献的结构属性,将有助于更好地理解结构-活性关系(SAR),并指导进一步设计具有生物活性的噻唑三唑。本文综述了噻唑三唑的生物活性,重点介绍了其在特定疾病条件下的SAR和药物靶点,这将有助于更好地理解支架,并将这些知识应用于未来噻唑三唑类药物的开发。
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引用次数: 0
Recent Advances in Bioconjugation of Aromatic Amino Acid Residues by a Reactivity-Guided Approach. 芳香族氨基酸残基生物偶联反应性研究进展。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-26 DOI: 10.1002/tcr.202500215
Bruno M da S Santos, Lívia C R M da Frota, Thais G Silva, Fernanda G Finelli

The bioconjugation of aromatic amino acids has emerged as a powerful strategy in chemical biology, drug discovery, and biomolecular research. Beyond the classical targeting of cysteine and lysine, aromatic amino acids residues offer higher selectivity owing to their lower abundance and critical roles in intermolecular interactions. Current synthetic approaches include substitution reactions, addition reactions, free-radical reactions, metal-catalyzed transformations, and biocatalytic approaches, enabling precise and versatile modifications in cells, tissues, and at the proteome level. In recent years, transition-metal catalysis and radical processes have dominated the field, with particular emphasis on tyrosine and tryptophan. This review provides a critical analysis of advances from the past 3 years, categorizing methodologies by reaction mechanism and highlighting how the intrinsic reactivity of aromatic amino acids can be harnessed for site-selective functionalization, ultimately expanding the accessible chemical space across all these residues.

芳香族氨基酸的生物偶联已成为化学生物学、药物发现和生物分子研究中的一种强有力的策略。除了传统的半胱氨酸和赖氨酸靶向外,芳香氨基酸残基由于其低丰度和在分子间相互作用中的关键作用而具有更高的选择性。目前的合成方法包括取代反应、加成反应、自由基反应、金属催化转化和生物催化方法,能够在细胞、组织和蛋白质组水平上进行精确和通用的修饰。近年来,过渡金属催化和自由基过程在该领域占据主导地位,特别是酪氨酸和色氨酸。这篇综述对过去3年的进展进行了批判性的分析,根据反应机理对方法进行了分类,并强调了如何利用芳香氨基酸的固有反应性进行选择性功能化,最终扩大了所有这些残基的可访问化学空间。
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引用次数: 0
Multifaceted Role of Oxalic Acid in Organic Synthesis: A Sustainable C1 and Hydrogen Surrogate for Catalytic Transformations. 草酸在有机合成中的多方面作用:一种可持续的催化转化的C1和氢替代品。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-26 DOI: 10.1002/tcr.202500226
Sheetal, Sandeep Kumar, Pralay Das

Transition-metal-catalyzed carbonylation and carboxylation reactions represents one of the dominant fields of synthetic chemistry, enabling the construction of structurally diverse and value-added carbonyl compounds. Although, different C1 surrogates have been developed to replace toxic carbon monoxide (CO), many of these require harsh acidic/basic conditions, metal catalysts, additives, or complex precursors, thereby generating substantial waste with lower atom economy. Herein, oxalic acid emanates as powerful multifaceted C1 synthon, capable of delivering CO, CO2, and H2 through clean, additive-free thermal decomposition. The decomposition profile not only enables in situ gas generation but also uniquely positions oxalic acid as both a carbonyl source and reducing agent. Herein, this account highlights the development of oxalic acid from a traditional reagent to strategically important platform in sustainable synthesis. Special emphasis is placed on development of oxalic acid-mediated protocols for functionalized carboxylic acids, ketones, alkynones, thioesters, bis(indolyl)methanes, formamides, heterocycles, and carbocycles synthesis. Furthermore, innovative reaction system designs including single- and dual-vial systems that employed oxalic acid as sustainable in situ and ex situ gaseous surrogate have also been highlighted. Overall, this article underscores the practical utility of oxalic acid as a bench-stable, cost-effective, and environmentally benign trifunctional reagent, paving way for next-generation carbonylation chemistry aligned with green synthetic principles.

过渡金属催化羰基化和羧基化反应是合成化学的主要领域之一,可以构建结构多样和高附加值的羰基化合物。虽然目前已经开发出不同的C1替代品来替代有毒的一氧化碳(CO),但许多替代品都需要苛刻的酸/碱条件、金属催化剂、添加剂或复杂的前体,从而产生大量的废物,原子经济性较低。在这里,草酸作为强大的多面C1合成体散发,能够通过清洁,无添加剂的热分解输送CO, CO2和H2。分解剖面不仅使原位产气成为可能,而且将草酸独特地定位为羰基源和还原剂。在这里,这篇文章强调了草酸从传统试剂到可持续合成的战略重要平台的发展。特别强调草酸介导的羧酸、酮、炔酮、硫酯、双(吲哚基)甲烷、甲酰胺、杂环和碳环合成方案的发展。此外,创新的反应系统设计,包括单瓶和双瓶系统,采用草酸作为可持续的原位和非原位气体替代物也得到了强调。总的来说,本文强调草酸作为一种稳定、经济、环保的三功能试剂的实际用途,为符合绿色合成原则的下一代羰基化化学铺平了道路。
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引用次数: 0
Hydrogen: Challenges and Opportunities for Storage and Transportation in the Clean Energy Economy. 氢:清洁能源经济中储存和运输的挑战和机遇。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-26 DOI: 10.1002/tcr.202500218
Buthaynah A Alqahtani, Hamid Zentou, Mahmoud M Abdelnaby, M Nasiruzzaman Shaikh

As a sustainable and clean energy source, hydrogen is gaining global recognition as a promising alternative to fossil fuels in the transition to a low-carbon economy. Its high energy density, versatility, and compatibility with renewable energy sources make it an attractive option for power generation, transportation, and industrial decarbonization. However, significant challenges hinder its widespread adoption, particularly in storage and transportation. Due to its low volumetric energy density, hydrogen requires advanced storage solutions such as chemical carriers, metal hydrides, compressed gas, and liquid hydrogen, each presenting unique financial and technological challenges. Additionally, transportation infrastructure-including pipelines and hydrogen carriers-must be further developed to enhance efficiency, improve safety, and minimize energy losses. Overcoming these challenges is essential to establishing a global hydrogen economy. Advancements in cost reduction, infrastructure development, and innovative storage materials are key to making hydrogen a viable mainstream energy source. This review highlights the critical barriers to hydrogen storage and transportation, while emphasizing the importance of continuous research, technological innovation, and supportive policies in accelerating the adoption of hydrogen for a cleaner, more sustainable energy future.

作为一种可持续的清洁能源,氢在向低碳经济转型的过程中,作为化石燃料的一个有前途的替代品,正在获得全球的认可。它的高能量密度、多功能性以及与可再生能源的兼容性使其成为发电、运输和工业脱碳的有吸引力的选择。然而,重大挑战阻碍了它的广泛采用,特别是在储存和运输方面。由于体积能量密度低,氢需要先进的存储解决方案,如化学载体、金属氢化物、压缩气体和液氢,每种都面临着独特的财务和技术挑战。此外,运输基础设施——包括管道和氢气载体——必须进一步发展,以提高效率、提高安全性,并最大限度地减少能源损失。克服这些挑战对于建立全球氢经济至关重要。成本降低、基础设施发展和创新存储材料的进步是使氢成为可行的主流能源的关键。本综述强调了氢储存和运输的关键障碍,同时强调了持续研究、技术创新和支持性政策在加速采用氢以实现更清洁、更可持续的能源未来方面的重要性。
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引用次数: 0
Advances in Modifying Carbon-Supported Single-Atom Nanozymes for Boosting Biosensing. 碳负载单原子纳米酶的生物传感改性研究进展。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-26 DOI: 10.1002/tcr.202500210
Jingjing Wei, Jianxuan Li, Hongyuan Shang

Carbon-based single-atom nanozymes (CB-SANzymes) have garnered significant attention in recent years due to their unique ability to mimic the active sites of natural enzymes. They exhibit not only maximized atom utilization efficiency but also strong metal-substrate interactions that effectively modulate the electronic structure of metal centers. Furthermore, carbon substrates facilitate rapid electron transfer during biosensing processes and enhance the stability of single-atom sites. These advantages make CB-SANzymes highly promising for biosensing applications. This review examines the fundamental properties of CB-SANzymes and discusses strategies for their modifications. Key strategies include increasing single-atom density, tuning the coordination environment, leveraging multimetal synergy, and engineering carbon substrates via heteroatom doping and defect construction. We also summarize the recent advances of CB-SANzymes in diverse biosensing platforms, such as colorimetric, fluorescent, and electrochemical systems. Their contribution to enhancing the sensitivity, selectivity, and accuracy of these systems is emphasized. Finally, current challenges and future prospects in the development and application of CB-SANzymes are discussed, with the aim of providing insightful guidance for further advancements in this rapidly evolving field.

碳基单原子纳米酶(CB-SANzymes)由于其独特的模仿天然酶活性位点的能力,近年来引起了人们的广泛关注。它们不仅表现出最大的原子利用效率,而且表现出强烈的金属-衬底相互作用,有效地调节金属中心的电子结构。此外,碳衬底促进了生物传感过程中的快速电子转移,提高了单原子位点的稳定性。这些优点使CB-SANzymes在生物传感应用中具有很大的前景。本文综述了CB-SANzymes的基本性质,并讨论了它们的修饰策略。关键策略包括增加单原子密度,调整配位环境,利用多金属协同作用,以及通过杂原子掺杂和缺陷构建来工程碳衬底。我们还总结了CB-SANzymes在不同生物传感平台上的最新进展,如比色、荧光和电化学系统。强调了它们对提高这些系统的灵敏度、选择性和准确性的贡献。最后,讨论了目前CB-SANzymes在开发和应用中的挑战和未来前景,旨在为这一快速发展的领域的进一步发展提供有洞察力的指导。
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引用次数: 0
Advancements in the Design and Development of Organic Fluorophores for the Excited State Intramolecular Proton Transfer Phenomenon 用于激发态分子内质子转移现象的有机荧光团的设计与开发进展。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-23 DOI: 10.1002/tcr.202500109
Gargi Mishra, Durgesh Singh, Surabhi Asthana, Himanshu Shekhar Tripathi, Rampal Pandey, Mrituanjay D. Pandey

Excited state intramolecular proton transfer (ESIPT) is a process where photoexcited molecules dissipate energy by transferring protons and undergoing tautomerization. With a brief introduction of a new emerging sensing mechanism, viz., CN isomerization, AIE, etc., this study explores the various aspects of ESIPT based on the current studies. Since Weller discovered ESIPT in salicylic acid and methyl salicylate, extensive research has developed on this topic, attributing to its wide applications. Here, it explores the structural and mechanical aspects of ESIPT and tautomerization.

激发态分子内质子转移(ESIPT)是光激发分子通过转移质子和发生互变异构来耗散能量的过程。本研究简要介绍了一种新兴的传感机制,即C - - N异构化,AIE等,并在现有研究的基础上对ESIPT的各个方面进行了探讨。自从韦勒在水杨酸和水杨酸甲酯中发现ESIPT以来,由于其广泛的应用,这一主题得到了广泛的研究。本文将探讨ESIPT和互变异构的结构和机械方面。
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引用次数: 0
Emerging Trends in Asymmetric Triazole Synthesis: from Click Chemistry to Biocatalysis. 不对称三唑合成的新趋势:从点击化学到生物催化。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-20 DOI: 10.1002/tcr.202500181
Suchandra Bhattacharjee, Arvind Singh Chauhan, Sujit Sarkar, Asit Kumar Das, Shubham Avinash Deshmukh

Triazole, also known as Pyrrolidazole, is a fundamental framework in heterocyclic chemistry. This is a five-membered aromatic compound consisting of three nitrogen atoms and two carbon atoms, which exist in two isomeric forms:1,2,3-triazole and 1,2,4-triazole. Both isomers exhibit a diverse range of applications across various domains, including materials science, medicinal chemistry, and catalysis. Despite their well-established advantages, triazole moieties are utilized as significant components in OLEDs, data storage devices, and organic photovoltaics. This review particularly emphasizes the recent advancements from 2020 to 2025, focusing on the asymmetric synthesis of triazole scaffolds and highlighting key methodologies ranging from copper-catalyzed azide-alkyne cycloaddition to biocatalytic strategies. Several studies have been reported about the development of innovative chiral ligands in conjunction with transition metals, including Ni, Rh, and Ir, leading to noble, efficient, and selective catalytic systems. Moreover, the present review article specifically explores the broad substrate scopes, reaction scalability, and detailed mechanistic insights that underscore the synthetic utility and versatility of these protocols. In addition, biocatalytic and chemoenzymatic approaches demonstrate the feasibility of sustainable and stereoselective synthesis of triazole-based antifungal agents. Overall, this mini-review not only guides the young researcher to develop new methodologies by carefully weighing their pros and cons but also equally assists the industrial scientist in designing bioactive heterocyclic compounds.

三唑,也被称为吡咯唑,是杂环化学的基本框架。这是一种五元芳香族化合物,由三个氮原子和两个碳原子组成,以两种异构体形式存在:1,2,3-三唑和1,2,4-三唑。这两种异构体在不同的领域都有不同的应用,包括材料科学、药物化学和催化。尽管三唑基团具有公认的优势,但它们在oled、数据存储设备和有机光伏电池中被用作重要的组成部分。本文重点介绍了2020年至2025年的最新进展,重点介绍了三唑支架的不对称合成,并重点介绍了从铜催化叠氮化物-炔环加成到生物催化策略的关键方法。一些研究已经报道了与过渡金属(包括Ni, Rh和Ir)结合的创新手性配体的发展,从而导致高贵,高效和选择性的催化体系。此外,本综述文章特别探讨了广泛的底物范围、反应可扩展性和详细的机制见解,强调了这些协议的合成效用和多功能性。此外,生物催化和化学酶的方法证明了可持续和立体选择性合成三唑类抗真菌药物的可行性。总的来说,这篇小型综述不仅指导年轻的研究人员通过仔细权衡其利弊来开发新方法,而且同样有助于工业科学家设计生物活性杂环化合物。
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引用次数: 0
The Brain as a Key Target and a Model for Iron-Loading by Bioactive Ferrocene-Based Compounds. Mini-Review. 脑作为生物活性二茂铁化合物铁负载的关键靶点和模型。本文着重。
IF 7.5 2区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2025-11-19 DOI: 10.1002/tcr.202500242
Lubov V Snegur

The present review outlines the latest advances in bio-organometallic ferrocene chemistry carried out on the brain. The brain has emerged as a key target and model for iron-loading by bioactive ferrocene-based compounds. This review focuses on the in vivo, ex vivo, and in vitro experimental data using ferrocene compounds in the brain, and discusses recent findings regarding their mechanisms of action. It also provides an overview of the biomedical aspects of studying ferrocene derivatives. The objective of this mini-review is to show the potential of ferrocene-modified compounds for studying brain challenges.

本文综述了脑内生物有机金属二茂铁化学研究的最新进展。大脑已成为生物活性二茂铁化合物加载铁的关键靶点和模型。本文综述了二茂铁化合物在大脑中的体内、离体和体外实验数据,并讨论了其作用机制的最新发现。它还提供了研究二茂铁衍生物的生物医学方面的概述。这篇小型综述的目的是展示二茂铁修饰化合物在研究大脑挑战方面的潜力。
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引用次数: 0
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