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Electrochemical carboxylation of α-fluoroalkyl cyclopropane with CO2 to mono- or difluoropentenoic acid α-氟烷基环丙烷与CO2的电化学羧化反应制单氟或二氟戊烯酸
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-23 DOI: 10.1039/d5qo00223k
Nan Feng, Mengmeng Jiang, Huimin Wang, Yuqing Zhong, Ying Sun, De-Yong Yang, Feng Zhou
{"title":"Electrochemical carboxylation of α-fluoroalkyl cyclopropane with CO2 to mono- or difluoropentenoic acid","authors":"Nan Feng, Mengmeng Jiang, Huimin Wang, Yuqing Zhong, Ying Sun, De-Yong Yang, Feng Zhou","doi":"10.1039/d5qo00223k","DOIUrl":"https://doi.org/10.1039/d5qo00223k","url":null,"abstract":"An electrochemical carboxylation of α-fluoroalkyl cyclopropanes with CO<small><sub>2</sub></small> is reported in this work. This approach constitutes a rare example of defluorinative carboxylation of organofluorine compounds with the simultaneous cleavage of C–F and C–C bonds. Accordingly, both α-CF<small><sub>2</sub></small>H and α-CF<small><sub>3</sub></small> cyclopropanes serve as effective substrates, facilitating the synthesis of pentenoic acids with <em>E</em>-configured monofluoroalkene or gem-difluoroalkene moiety with high chemo- and stereoselectivity. The reaction can be also performed under a nonsacrificial anode system. The synthetic practicality is further highlighted by the diverse functionalizations of the resulting multifunctional fluorinated acids. Cyclic voltammetry studies were performed to provide mechanistic insights into the reaction’s origins.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"8 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143862553","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Total Synthesis and Stereochemical Assignment of Cubensci Acid 古bensci酸的全合成及立体化学配位
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-23 DOI: 10.1039/d5qo00545k
Yangyang Jiang, Junyang LIU, Tao Ye
{"title":"Total Synthesis and Stereochemical Assignment of Cubensci Acid","authors":"Yangyang Jiang, Junyang LIU, Tao Ye","doi":"10.1039/d5qo00545k","DOIUrl":"https://doi.org/10.1039/d5qo00545k","url":null,"abstract":"The absolute configuration of cubensic acid was predicted using the “Biochemistry-based Rule” and confirmed through total synthesis. Key steps in the synthesis included a titanium-mediated aldol reaction, a Paterson anti-aldol reaction, and a vinylogous Mukaiyama aldol reaction.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"181 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143862648","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A General Protocol for Efficient Construction of Perfluoro-tert-butyl Alkynes with (Perfluoro-tert-butyl)propiolic Acid 用（全氟叔丁基）丙酸高效构造全氟叔丁基炔的一般方案
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-23 DOI: 10.1039/d5qo00601e
Zhiqiang Wei, Guangxing Gu, Wei Zhang, Yanchuan Zhao, Jinbo Hu
{"title":"A General Protocol for Efficient Construction of Perfluoro-tert-butyl Alkynes with (Perfluoro-tert-butyl)propiolic Acid","authors":"Zhiqiang Wei, Guangxing Gu, Wei Zhang, Yanchuan Zhao, Jinbo Hu","doi":"10.1039/d5qo00601e","DOIUrl":"https://doi.org/10.1039/d5qo00601e","url":null,"abstract":"The perfluoro-tert-butyl group (PFtB) stands out, in part, due to its unparalleled analytical capabilities, as an indispensable functional group for sensing and imaging within biological systems. Although previously we have accomplished the introduction of perfluoro-tert-butyl group to sp3-and sp2-carbons, the perfluoro-tert-butylation of sp-carbon remains a challenging task. In this study, we develop a versatile method to construct structurally diverse PFtB-substituted alkynes, utilizing (perfluoro-tert-butyl)propiolic acid (PFtPA) as a new reagent. PFtPA is easy to synthesize and can undergo Pd/Cucatalyzed decarboxylative coupling with a wide array of (aryl, alkyl, alkenyl, and alkynyl) halides and triflates. This synthetic protocol is not only high-yielding but also compatible with various functional groups. Furthermore, we demonstrate the potential of this new synthetic protocol by developing a 19F-labeled probe that is proficient in distinguishing analytes with distal chiral centers.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"108 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143862651","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Catalytic enantioselective divergent reaction of thioimidates with naphthols: construction of N,S-acetal-containing tetrasubstituted carbon centers 硫代亚胺酸盐与萘酚的催化对映选择性歧化反应：构建含 N,S-缩醛的四代碳中心
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-22 DOI: 10.1039/d5qo00430f
Qiao-Qiao Peng, Xing Yang, Xi-Sha Xue, Juan Liao, Lei Yang, Yong You, Zhen-Hua Wang, Lili Zhao, Wei-Cheng Yuan, Jian-Qiang Zhao
{"title":"Catalytic enantioselective divergent reaction of thioimidates with naphthols: construction of N,S-acetal-containing tetrasubstituted carbon centers","authors":"Qiao-Qiao Peng, Xing Yang, Xi-Sha Xue, Juan Liao, Lei Yang, Yong You, Zhen-Hua Wang, Lili Zhao, Wei-Cheng Yuan, Jian-Qiang Zhao","doi":"10.1039/d5qo00430f","DOIUrl":"https://doi.org/10.1039/d5qo00430f","url":null,"abstract":"Enantiopure N,S-acetals are distributed in numerous natural products and pharmaceuticals, exhibiting a broad spectrum of biological activities. Herein we open a new avenue for accessing N,S-acetal-containing tetrasubstituted carbon stereogenic centers through an enantioselective divergent reaction between cyclic α-carbonyl thioimidates and naphthols. Using 2-naphthols as nucleophilic partners, the reaction enabled the formation of structurally diverse furanonaphthobenzo[b]thiophene derivatives bearing two vicinal diheteroatom-containing tetrasubstituted carbon stereogenic centers with high optical purities through a domino aza-Friedel–Crafts/O-hemiacetalization of the exocyclic C=O bond. In contrast, the enantioselective addition of1-naphthols/electron-rich phenols to cyclic α-carbonyl thioimidates led to the formation of N,S-acetal-containing tetrasubstituted carbon stereogenic centers in high yields and excellent enantioselectivities. DFT studies provide valuable insights into the reaction mechanism and the origin of enantioselectivity, as well as the reaction divergence observed with 2-naphthols and 1-naphthols, respectively. The results suggest that the C–C bond formation during the addition of naphthols to thioimidates is the enantioselectivity-determining step, while the rate-determining step is the C–H bond cleavage. Additionally, both kinetically and thermodynamically, the reaction with 2-naphthols favors the subsequent O-hemiacetalization to yield cyclization products, whereas the addition of 1-naphthols to thiomidates is thermodynamically driven for the synthesis of chiral N,S-acetals through the subsequent protonation process.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"219 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143857583","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Oxetane as a part of modern medicinal chemistry toolbox: the advanced synthesis of 3,3-disubstituted building blocks Oxetane作为现代药物化学工具箱的一部分：3,3-二取代构建块的高级合成
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-22 DOI: 10.1039/d5qo00572h
Eduard V. Litskan, Oleksandr V. Semenchenko, Serhii V. Lynnyk, Dmitry Granat, Bohdan V. Vashchenko, Anastasiia Ye. Hoida, Daria A. Tolmachova, Dmitry Alexandrovich Lega, Oleksandr O Grygorenko, Dmitriy M. Volochnyuk, Serhiy V. Ryabukhin
{"title":"Oxetane as a part of modern medicinal chemistry toolbox: the advanced synthesis of 3,3-disubstituted building blocks","authors":"Eduard V. Litskan, Oleksandr V. Semenchenko, Serhii V. Lynnyk, Dmitry Granat, Bohdan V. Vashchenko, Anastasiia Ye. Hoida, Daria A. Tolmachova, Dmitry Alexandrovich Lega, Oleksandr O Grygorenko, Dmitriy M. Volochnyuk, Serhiy V. Ryabukhin","doi":"10.1039/d5qo00572h","DOIUrl":"https://doi.org/10.1039/d5qo00572h","url":null,"abstract":"Despite numerous potential advantages of oxetanes, their restricted synthetic accessibility and propensity to ring-opening hamper their wide application in drug design. In this work, we disclose our experimental achievements and 10 years of experience in oxetane chemistry and provide a comprehensive study on the oxetane core tolerance towards the reaction conditions of the typical toolbox of organic and medicinal chemists, which is based on our original, unpublished developments. The scope of examined reactions includes oxidation, reduction, alkylation, acylation, nucleophilic substitu-tion, C–C/C=C/C≡C bond formation, hydrolysis, and protecting groups cleavage, and demonstrates the stability of the oxetane's moiety towards acidic and basic conditions. Over 40 transformations were applied to generate the oxetane chemical stability profile, which could direct the design of other synthetic approaches for the synthesis and incorporation of oxetanes in the future. The additional aim of the work included the optimization of the synthetic protocols with the possibility of scaling up to 1 kg in a single run. Newly designed synthetic protocols in our hands allowed for the prepara-tion of novel 3,3-disubstituted oxetanes as small building blocks (over 100 examples, almost 90% of which were not reported previously in the literature). These results benefit the development of oxetanes as a part of the toolbox of modern medicinal chemistry, as well as their incorporation into drug development programs.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"24 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143862519","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Green and modular synthesis of azepino[4,3,2-cd]indoles and diazepino[6,5,4-cd]indoles via hydride transfer-involved cascade cyclization in ethanol 乙醇中氢化物转移级联环化绿色模块化合成氮平[4,3,2-cd]吲哚和二氮平[6,5,4-cd]吲哚
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-22 DOI: 10.1039/d5qo00058k
Qian-Hao Zhuang, Xiao-Lin Wang, Wei Gao, Bin Qiu, Xiao-De An, Houchen Wang, Yao-Bin Shen, Jian Xiao
{"title":"Green and modular synthesis of azepino[4,3,2-cd]indoles and diazepino[6,5,4-cd]indoles via hydride transfer-involved cascade cyclization in ethanol","authors":"Qian-Hao Zhuang, Xiao-Lin Wang, Wei Gao, Bin Qiu, Xiao-De An, Houchen Wang, Yao-Bin Shen, Jian Xiao","doi":"10.1039/d5qo00058k","DOIUrl":"https://doi.org/10.1039/d5qo00058k","url":null,"abstract":"The modular synthesis of high-value azepino[4,3,2-cd]indole and its analogs from versatile synthons and readily available feedstocks has been a challenging project. Herein, we report the 1,6-hydride transfer-involved cascade [6 + 1] cyclization of 4-dialkylamino-indole-3-carbaldehydes with diverse 1C,1C- and 1N,1N -bisnucleophiles in ethanol, enabling the green and modular synthesis of diazepino[6,5,4-cd]indoles and diazepino[6,5,4-cd]indoles. This method highlights catalyst-free redox-neutral conditions, excellent substrate compatibility, simple operational procedures, gram-scale synthesis, and diverse product derivatization.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"29 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143862654","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Bifunctional iron-mediated multicomponent Markovnikov-selective radical hydrothiolation of alkenes 双功能铁介导的多组分马尔可夫尼科夫选择性自由基氢硫基化烯烃
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-22 DOI: 10.1039/d5qo00308c
Yi-Nuo Wang, Hongyu Jia, Lan Yao, Yu Chen, Han-Le Liu, Fengbing Liang, Dexin Feng, Da-Zhen Xu
{"title":"Bifunctional iron-mediated multicomponent Markovnikov-selective radical hydrothiolation of alkenes","authors":"Yi-Nuo Wang, Hongyu Jia, Lan Yao, Yu Chen, Han-Le Liu, Fengbing Liang, Dexin Feng, Da-Zhen Xu","doi":"10.1039/d5qo00308c","DOIUrl":"https://doi.org/10.1039/d5qo00308c","url":null,"abstract":"Direct (utilizing easily available and abundant raw materials) and selective hydrofunctionalization of alkenes is an appealing method for simplifying chemical synthesis. Dithiocarbamates have gained increasing prominence in medicine and agrochemistry. Herein, we report an iron-mediated multicomponent Markovnikov hydrothiolation of alkenes to afford dithiocarbamates with good yields. This mild strategy avoids the preparation of thiolation reagents and shows excellent functional group tolerance. The synthetic utility of this transformation was demonstrated by gram-scale synthesis and late-stage modification of various drug and bioactive molecules. Mechanistic studies show that the reaction involves an iron catalyzed hydrogen atom transfer and a single electron transfer process. Iron salts play a dual role, hitting two birds with one stone.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"7 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143857584","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Machine learning-guided protein engineering to improve the catalytic activity of transaminases under neutral pH conditions 以机器学习为指导的蛋白质工程改善转氨酶在中性pH值条件下的催化活性
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-22 DOI: 10.1039/d5qo00423c
Si-Han Liu, Ligai Bai, Xu-Dong Wang, Qi-Qiang Wang, De-Xian Wang, Uwe T. Bornscheuer, Yu-Fei Ao
{"title":"Machine learning-guided protein engineering to improve the catalytic activity of transaminases under neutral pH conditions","authors":"Si-Han Liu, Ligai Bai, Xu-Dong Wang, Qi-Qiang Wang, De-Xian Wang, Uwe T. Bornscheuer, Yu-Fei Ao","doi":"10.1039/d5qo00423c","DOIUrl":"https://doi.org/10.1039/d5qo00423c","url":null,"abstract":"Biocatalysis provides an eco-friendly and efficient method for the synthesis of fine chemicals, pharmaceuticals, and biofuels. However, the catalytic performance of enzymes is greatly reduced when they react under non-optimal pH conditions. Despite efforts in protein engineering to improve enzymatic pH dependence, predicting and optimizing catalytic activity under various pH conditions remains challenging. Recent advancements in machine learning (ML) provide a promising solution by enabling data-driven predictions of enzyme properties, thus reducing the need for labor-intensive experiments. This study aims to enhance enzyme activity and regulate pH dependence through ML-guided protein engineering. Using a transaminase from <em>Ruegeria</em> sp. TM1040 as mutation template, we first collected high-quality experimental data from a series of variants by measuring their activity at a series of pH conditions. Based on this, we developed a ML model to predict catalytic activity under different pH conditions. This work provides a powerful ML tool to guide the rational design of variants, which showed improved activity (up to 3.7-fold comparing to starting variant) at pH 7.5 condition, and offers a data-driven protein engineering strategy to achieve co-optimization of enzyme activity and pH dependence, demonstrating the potential of ML to accelerate enzyme engineering for industrial applications","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"58 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143857513","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Quinoline Derivatives by Palladium-Catalyzed Isocyanide Insertion/Undirected C(sp²)-H Functionalization/[4+1] Cyclization Reactions Involving Aryl Isocyanide 钯催化异氰酸芳基插入/无向C（sp²）-H功能化/[4+1]环化反应合成喹啉衍生物
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-17 DOI: 10.1039/d5qo00349k
Shan-Shan Liu, Yong-Jie Wu, Jiang-Nan Zheng, Zhi-Lin Ren, Shao-Jie Jiang, Jun Wu, Ke-Ji Li, Ping He, Long Wang
{"title":"Synthesis of Quinoline Derivatives by Palladium-Catalyzed Isocyanide Insertion/Undirected C(sp²)-H Functionalization/[4+1] Cyclization Reactions Involving Aryl Isocyanide","authors":"Shan-Shan Liu, Yong-Jie Wu, Jiang-Nan Zheng, Zhi-Lin Ren, Shao-Jie Jiang, Jun Wu, Ke-Ji Li, Ping He, Long Wang","doi":"10.1039/d5qo00349k","DOIUrl":"https://doi.org/10.1039/d5qo00349k","url":null,"abstract":"The study reports a novel palladium-catalyzed diaryl isocyanide insertion reaction strategy, which has opened up a brand-new avenue for the efficient synthesis of quinoline derivatives. The remarkable features of this method are manifested in two aspects. On the one hand, it ingeniously utilizes the palladium catalyst to directly and highly selectively activate the C(sp²)-H bonds of aromatic substrates, demonstrating excellent chemoselectivity. On the other hand, by ingeniously integrating the C(sp²)-H functionalization reaction with the [4 + 1] cyclization reaction in the same reaction system, this method significantly simplifies the synthesis steps and achieves the goal of directly constructing quinoline derivatives in just one step from simple and readily available starting materials. This study has not only greatly enriched the synthetic strategy library of quinoline chemistry but also provided solid support for scientific research in related fields.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"34 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143842001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Carboxylation of C(sp2)−H bonds in quinolone derivatives with CO2: Facile synthesis of quinolone carboxylic acids 喹诺酮类衍生物中C(sp2)−H键与CO2的羧基化：喹诺酮类羧酸的简易合成
IF 5.4 1区 化学
Organic Chemistry Frontiers Pub Date : 2025-04-16 DOI: 10.1039/d5qo00491h
Changfu Li, Wei Zhang, Yunyi Xu, Yang Su, Tian-Yu Gao, Jian-Heng Ye, Lei Song, Da-Gang Yu
{"title":"Carboxylation of C(sp2)−H bonds in quinolone derivatives with CO2: Facile synthesis of quinolone carboxylic acids","authors":"Changfu Li, Wei Zhang, Yunyi Xu, Yang Su, Tian-Yu Gao, Jian-Heng Ye, Lei Song, Da-Gang Yu","doi":"10.1039/d5qo00491h","DOIUrl":"https://doi.org/10.1039/d5qo00491h","url":null,"abstract":"Quinolone carboxylic acids and derivatives are widely regarded as privileged scaffolds due to their broad-spectrum biological activities. Herein, we report a direct and efficient carboxylation of C(sp2)−H bonds in quinolone derivatives with CO2. This work offers a highly atom- and step-economical approach to a variety of quinolone-3-carboxylic acids and derivatives with good yields. Moreover, this methodology provides a convenient route to access both marketed drugs and other bioactive molecules. Notably, the derived glycogen synthase kinase 3β (GSK-3β) inhibitor VP0.7 exhibits promising cytotoxic activity against several cancer cell lines, highlighting its potential application in drug discovery.","PeriodicalId":97,"journal":{"name":"Organic Chemistry Frontiers","volume":"1 1","pages":""},"PeriodicalIF":5.4,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143837499","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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