Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-10-21DOI: 10.1016/j.tetlet.2025.155868
Na Wang , Xilan Jiang , Yujiao He , Mengqi Wang , Yuanwei You , Yufei Che , Dexiu Cui , Hongbo Dong
{"title":"First total synthesis of acronyculatin S","authors":"Na Wang , Xilan Jiang , Yujiao He , Mengqi Wang , Yuanwei You , Yufei Che , Dexiu Cui , Hongbo Dong","doi":"10.1016/j.tetlet.2025.155868","DOIUrl":"10.1016/j.tetlet.2025.155868","url":null,"abstract":"<div><div>Acronyculatin S is a naturally occurring benzofuran derivative isolated from <em>Acronychia pedunculata</em> and has been reported to exhibit antibacterial activity. In this study, the first total synthesis of acronyculatin S was achieved through a concise and scalable route involving a Friedel–Crafts acylation, a Sonogashira coupling, and an europium(III)-catalyzed Claisen rearrangement as key steps. However, antibacterial evaluation of the synthetic sample against a panel of Gram-positive bacterial strains revealed no significant inhibitory activity under the tested conditions (MIC > 64 μg/mL). This work provides a reliable synthetic route for accessing acronyculatin S and related analogues, facilitating further studies on the chemical and biological properties of this class of natural products.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155868"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145361382","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-10-17DOI: 10.1016/j.tetlet.2025.155852
Raja Abdul Basit , Shaziya Hassan , Bilal A. Bhat
{"title":"Micelle-enabled synthesis of diverse 3-substituted-3H-benzo[f]chromene constructs in water","authors":"Raja Abdul Basit , Shaziya Hassan , Bilal A. Bhat","doi":"10.1016/j.tetlet.2025.155852","DOIUrl":"10.1016/j.tetlet.2025.155852","url":null,"abstract":"<div><div>We have developed an interesting strategy to target a range of benzo[<em>f</em>]chromene constructs in water, which aligns with the green and sustainable chemistry ideas. The approach involves the reaction of β-naphthols with enals to furnish benzochromene constructs through a diverted reaction pathway in micellar medium compared to the reaction in conventional organic solvents. This transformation occurs within the CPB-micellar nanoreactors through the condensation of β-naphthols with enals, followed by the diene-enone electrocyclization reaction to steer benzo[<em>f</em>] chromene scaffolds in great precision.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155852"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145361386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-10-31DOI: 10.1016/j.tetlet.2025.155875
Vittal Seema , Murali Mohan Achari Kamsali , Laxman Mahadev Alakonda , Ravi Varala , Mohamed Hussein , Mohammed Mujahid Alam
{"title":"Mini-update on the applications of Hypophosphites in organic synthesis with a special focus on sodium hypophosphite (NaH2PO2)","authors":"Vittal Seema , Murali Mohan Achari Kamsali , Laxman Mahadev Alakonda , Ravi Varala , Mohamed Hussein , Mohammed Mujahid Alam","doi":"10.1016/j.tetlet.2025.155875","DOIUrl":"10.1016/j.tetlet.2025.155875","url":null,"abstract":"<div><div>Sodium hypophosphite (NaH₂PO₂) is an inexpensive, abundant, and environmentally friendly reagent widely used in organophosphorus synthesis. Its stability, low toxicity, and ease of handling make it a versatile “green” phosphorus source. This mini-review highlights recent developments (2019–2025) in its applications, including as a phosphorus donor, reducing agent, catalyst, deuterio-deiodinating agent, and deoxyamination reagent. Related reagents such as H₃PO₂ and Ca(H₂PO₂)₂ are also briefly discussed. Mechanistic insights are provided where relevant, alongside the advantages and limitations of current methodologies. This concise overview aims to guide researchers in harnessing hypophosphite reagents for efficient and sustainable organic synthesis.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155875"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145463895","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-11-15DOI: 10.1016/j.tetlet.2025.155895
Peng Xu , Xu-Long Qin
{"title":"Recent advances in electrochemical earth-abundant metal catalysis for CX (X = C, N, O) bond formation via bidentate directing groups","authors":"Peng Xu , Xu-Long Qin","doi":"10.1016/j.tetlet.2025.155895","DOIUrl":"10.1016/j.tetlet.2025.155895","url":null,"abstract":"<div><div>Organic electrochemistry has attracted increasing attention as a novel strategy to replace traditional chemical oxidants and reductants in organic synthesis, thereby avoiding employing stoichiometric amounts of toxic reagents. In particular, electrochemical transition metal-catalyzed C<img>H functionalization assisted by bidentate directing groups provides an efficient and straightforward approach for transforming abundant organic molecules into various functional groups. This review summarizes recent advances in electrochemical, transition-metal-catalyzed C<img>H functionalization mediated by bidentate directing groups, focusing on C<img>X (X = C, N, O) bond formation.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155895"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145576487","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-11-14DOI: 10.1016/j.tetlet.2025.155900
Qing Wei , Ping Ying , Yunpeng Sun , Mengmeng Yu , Letian Cui , Xiaoli Sun , Qiang Zheng , Lingyi Kong , Jun Luo
{"title":"Two new trinortriterpenoids from Munronia unifoliolata","authors":"Qing Wei , Ping Ying , Yunpeng Sun , Mengmeng Yu , Letian Cui , Xiaoli Sun , Qiang Zheng , Lingyi Kong , Jun Luo","doi":"10.1016/j.tetlet.2025.155900","DOIUrl":"10.1016/j.tetlet.2025.155900","url":null,"abstract":"<div><div>Mufolinoids W and X (<strong>1</strong> and <strong>2</strong>), two new trinortriterpenoids, along with their biosynthetic precursor triterpenoids (<strong>3</strong> and <strong>4</strong>), were isolated and identified from the medicinal plant <em>Munronia unifoliolata</em> Oliv.—a species used in Traditional Chinese Medicine for treating rheumatic arthritis pain and traumatic injuries. Their structures were identified by high-resolution mass spectrometry (HR-MS), one-dimensional/two-dimensional nuclear magnetic resonance (1D/2D NMR), and experimental and calculated electronic circular dichroism (ECD) methods. Structurally, <strong>1</strong> and <strong>2</strong> were the second example of 3/4-seco trinortriterpenoids from the plant kingdom. Biologically, the inhibitory effects of <strong>1</strong> and <strong>2</strong> on nitric oxide (NO) production and their multidrug resistance reversal activity were evaluated and screened.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155900"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145576585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-11-10DOI: 10.1016/j.tetlet.2025.155896
Ying Xie , Lixu You , Yi Liu , Yinlong Lai
{"title":"Isothiourea-catalyzed addition of aryl acetates to vinylogous imine intermediates generated in situ from arylsulfonyl indoles","authors":"Ying Xie , Lixu You , Yi Liu , Yinlong Lai","doi":"10.1016/j.tetlet.2025.155896","DOIUrl":"10.1016/j.tetlet.2025.155896","url":null,"abstract":"<div><div>Indole propionates are essential precursors for the construction of indole-propionic acid with TRPC6 inhibitory activity. Herein, we developed a novel approach to multisubstituted indole propionates via isothiourea-catalyzed addition of aryl acetates to vinylimine intermediates, which are generated in situ from arylsulfonyl indoles under mild conditions. This new method features a broad substrate scope and good yields. Importantly, it enabled us to complete the concise syntheses of indole-propionic acid with TRPC6 inhibitory activity through the hydrolysis of indole propionate.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155896"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145525927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-11-03DOI: 10.1016/j.tetlet.2025.155874
T'ea P. Cameron , Tamam El-Elimat , Sonja L. Knowles , Huzefa A. Raja , Jacques Fournier , Steven P. Maher , Dennis E. Kyle , Nicholas H. Oberlies
{"title":"Soudanones H and I from a freshwater fungus Hongkongmyces sp.","authors":"T'ea P. Cameron , Tamam El-Elimat , Sonja L. Knowles , Huzefa A. Raja , Jacques Fournier , Steven P. Maher , Dennis E. Kyle , Nicholas H. Oberlies","doi":"10.1016/j.tetlet.2025.155874","DOIUrl":"10.1016/j.tetlet.2025.155874","url":null,"abstract":"<div><div>Two new compounds were isolated from a freshwater fungus [<em>Hongkongmyce</em>s sp. (strain G892)] by bioactivity-directed fractionation against <em>Plasmodium falciparum</em>. The structures of <strong>1</strong> and <strong>2</strong> were elucidated with the use of HRMS and NMR data, and their absolute configurations were identified by ECD spectroscopy. Compound <strong>1</strong> was evaluated for antiplasmodial activity against <em>P. falciparum</em> and cytotoxicity against human liver cancer cell lines.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155874"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145463892","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Nitro radical addition and cyclization of 1,5-enenitriles for making pyrrolidine-2,4-diones","authors":"Mifei Yu, Wentao Shao, Lingfeng Luo, Yue Zhang, Shenghu Yan, Jia-Yin Wang, Xiaoming Ma","doi":"10.1016/j.tetlet.2025.155881","DOIUrl":"10.1016/j.tetlet.2025.155881","url":null,"abstract":"<div><div>A mild and efficient method for the nitro radical-mediated addition and cyclization of <em>N</em>-tethered 1,5-enenitriles is presented. Utilizing commercially available <em>tert</em>-butyl nitrite (<em>t-BuONO</em>) as a practical nitro radical source, this transformation enables the straightforward synthesis of a diverse range of nitro-substituted pyrrolidine-2,4-dione derivatives. The reaction proceeds under metal-free conditions, exhibits broad substrate scope, and offers operational simplicity, highlighting its potential for rapid access to pharmacologically relevant scaffolds.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155881"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145463893","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-11-04DOI: 10.1016/j.tetlet.2025.155877
Fereshteh Khorasani, Reza Ranjbar-Karimi
{"title":"Synthesis of new cluster compounds of triazoles containing perhalogenated azides and mono-, tri-perhalopropargyl cores as cages or hostage","authors":"Fereshteh Khorasani, Reza Ranjbar-Karimi","doi":"10.1016/j.tetlet.2025.155877","DOIUrl":"10.1016/j.tetlet.2025.155877","url":null,"abstract":"<div><div>Herein, we introduce novel triazole compounds comprising a perhalopyridine (PFP or PCP) core as the host with a perhalogenated azide. The S<sub>N</sub>Ar reactions of pentafluoropyridine at positions 4, 2, 6, and two positions 4, 2 were evaluated. Ultimately, a concise synthetic approach utilizing copper-promoted click chemistry (CuAAC) was employed to prepare a library of structurally diverse mono-, di, and tri-1,4-disubstituted-1,2,3-triazoles moieties of (fluoro-chloro) aryl. The chemical structures of the produced compounds were confirmed using various techniques such as FT-IR and NMR spectroscopy.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155877"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145526005","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Tetrahedron LettersPub Date : 2026-01-15Epub Date: 2025-10-30DOI: 10.1016/j.tetlet.2025.155876
Durgesh Sarothiya, Abhinay S. Chillal, Umesh A. Kshirsagar
{"title":"HFIP-promoted one-pot synthesis of (Pyrazolo[1,5-a]pyrimidinyl)(indolyl)methanes using Rongalite as a C1 synthon under mild conditions","authors":"Durgesh Sarothiya, Abhinay S. Chillal, Umesh A. Kshirsagar","doi":"10.1016/j.tetlet.2025.155876","DOIUrl":"10.1016/j.tetlet.2025.155876","url":null,"abstract":"<div><div>In this report, we established an efficient synthetic strategy for the construction of heterodiarylmethanes via the coupling of pyrazolo[1,5-<em>a</em>]pyrimidine and indole using rongalite as methylene source under metal-free conditions at room temperature in HFIP solvent. Rongalite was used as a relatively benign and metal-free reagent and cost-effective C1 synthon. The present methodology offers a total of 21 examples, moderate to good yields of products and easy operations under the mild conditions. The newly synthesized molecules represent a unique class of functionalized heterocycles with potential biological relevance.</div></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":"174 ","pages":"Article 155876"},"PeriodicalIF":1.5,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145463891","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}